Dasatinib

Catalog No.S1021

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.

Price Stock Quantity  
USD 140 In stock
USD 147 In stock
USD 370 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Dasatinib Chemical Structure

Dasatinib Chemical Structure
Molecular Weight: 488.01

Validation & Quality Control

Cited by 62 publications:

10 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Src Inhibitors with Unique Features

  • Pan Src Inhibitor

    Saracatinib (AZD0530) Pan-Src inhibitor, IC50=2.7-11 nM for c-Src/c-Yes/Fyn/Lyn/Blk/Fgr/Lck.

  • FDA-approved Src Inhibitor

    Bosutinib (SKI-606) Approved by FDA for Ph+ chronic myelogenous leukemia (CML).

  • Newest Src Inhibitor

    PP1 Potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • Classic Src Inhibitor

    KX2-391 The first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Product Information

  • Compare Src Inhibitors
    Compare Src Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
Targets Abl [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
c-Kit (D816V) [2]
(Cell-free assay)
c-Kit (wt) [2]
(Cell-free assay)
IC50 0.6 nM 0.8 nM 37 nM 79 nM
In vitro Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. Dasatinib has a two-log (∼325-fold) increased potency relative to imatinib. Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range. Dasatinib directly targets wild-type and mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl. [1] The percent of colonies of TgE bone marrow cells are decreased from 100% in untreated wells to 4.12% in Dasatinib treated wells. In the presence of Dasatinib, the difference in the percentage of colonies formed by WT and TgE bone marrow cells is statistically significant. Expression of LMP2A is able to promote B lymphocyte survival and proliferation, which can be inhibited by targeting Lyn and/or c-Abl kinases through Dasatinib. [3] Dasatinib treatment inhibits Src signaling, decreases growth, and induces cell cycle arrest and apoptosis in a subset of thyroid cancer cells. Treatment with increasing doses of Dasatinib (0.019 μM to 1.25 μM) for 3 days inhibits the growth of the C643, TPC1, BCPAP, and SW1736 cell lines by about 50% at low nanomolar concentrations, while higher concentrations are required to inhibit the growth of the K1 cell line. Treatment with 10 nM or 50 nM Dasatinib results in a 9-22% increase of cells in the G1 population among BCPAP and SW1736 and K1 cells, and a corresponding 7-18% decrease in the percentage of cells in the S phase. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
M07ep210MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3SzN|czKGh?MYLEUXNQMXrJR|UxRTBwMECwNFch|ryPNXThdm16OTd7NU[wPFA>
K562NGjwSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFr1fI44OiCqMX\EUXNQM4T6OGlEPTB;MD6wNFEh|ryPMn2wNVc6PTZyOEC=
M07eMkexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmfkO|IhcA>?MofpSG1UVw>?NF\NNY1KSzVyPUCuNFAyOiEQvF2=MUixO|k2PjB6MB?=
ALL3MVXDfZRwfG:6aXOgRZN{[Xl?MlzYNE4y|ryPMV[3NkBpNET6ZmdFVVORM4jpN2lEPTB;MD6wNFA1KM7:TR?=MX2xPVg5QTV2MB?=
CMLM1zRd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2fy[|IxKG2rbh?=M1ztbGROW09?MmDwTWM2OD1yLkCwNUDPxE1?M3\jU|E6OjF7MEG2
BA/F3NXmxSIxVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NV3ad4FIPzJiaB?=MnG2SG1UVw>?M17k[2lEPTB;Nj61PFkh|ryPNX7F[4NjOjNyOEi2OFQ>
BA/F3NF\wfHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MVO3NkBpNVqwemluTE2VTx?=MnfPTY5lfWOnczDhcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDL1[zJINmdGy|IHX4dJJme3OrbnegRoNzNUGkbDDNN|UyXCCvdYThcpQhf2m2aDDJR|UxKG:oIECuNFAxQDQQvF2=MmrZNlMxQDh4NES=
BA/F3MkHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlryO|IhcA>?MmPESG1UVw>?M2roUWlv\HWlZYOgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQT;GN{Bk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBD[3JvQXLsJJdqfGhiSVO1NEBw\iByLkCwOFXPxE1?M2\rSFI{ODh6NkS0
BA/F3M{fYemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkDNO|IhcA>?MUHEUXNQMkn3TY5lfWOnczDhcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDL1[zJINmdGy|IHX4dJJme3OrbnegRoNzNUGkbDDUN|E2USCvdYThcpQhf2m2aDDJR|UxKG:oIEGuO|E1|ryPMVeyN|A5QDZ2NB?=
BA/F3MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYW3NkBpM3K1XWROW09?M3;CTmlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKEZ2OE\TJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFA6|ryPNUPNTnBbOjN|MEG3NFM>
BA/F3NFLld3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NV\zXZQ{PzJiaB?=M2fCcmROW09?NH3zcHRKdmS3Y3XzJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiQlPSMWFDVCCHMkW1T{BufXSjboSgZZN{\XO|ZXSgZZMh\3Kxd4ToJGlvcGmkaYTpc44hf2m2aDDJR|UxKG:oIECuNFA{Os7:TR?=NWrK[XYyOjN|MEG3NFM>
BA/F3MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnnmO|IhcA>?MV7EUXNQM3jLVGlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKEd{NUDFJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFUy|ryPNEHuUHczOzNyMUewNy=>
BA/F3MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXnFWpJ6PzJiaB?=MVPEUXNQNXL2[oFMUW6mdXPld{BkgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFLDVk1CSkxiUUK1NmghdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBKdmirYnn0bY9vKHerdHigTWM2OCCxZjCwMlAxQM7:TR?=MXSyN|MxOTdyMx?=
BA/F3MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmLxO|IhcA>?NG\MVoFFVVORM3nOPGlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKEV|NUnWJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFE{|ryPMXSyN|MxOTdyMx?=
BA/F3MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWL1[mRrPzJiaB?=MkT4SG1UVw>?Mmj1TY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCEQ2KtRWJNKGG|c3Xzd4VlKGG|IHfyc5d1cCCLbnjpZol1cW:wIIfpeIghUUN3MDDv[kAxNjByMUpOwG0>Mlq2NlM{ODF5MEO=
BA/F3NYTLbJl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF\PUXM4OiCqNVfLOHBNTE2VTx?=M2\yUWlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKFl{NUPIJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFI{|ryPNUfhOVV7OjN|MEG3NFM>
BA/F3MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFPJbYs4OiCqM2j2cGROW09?MY\JcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4PpcochSkOULVHCUEBVOzF3STDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIFnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDNwNt88US=>M3ry[|I{OzBzN{Cz
BA/F3Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHfWcVM4OiCqM13semROW09?MVrJcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBKdmirYnn0bY9vKHerdHigTWM2OCCxZjCyMlXPxE1?M{TOPVI{OzBzN{Cz
T cellM2D5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2TBPVczKGh?M3HZc2ROW09?M{\2bmlvcGmkaYTzJIFvfGliQ1SzMUBidmRiYX70bUBETDJ6LXnu[JVk\WRiVDDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDBwMECz{txOMnnUNVcyPTR3MUK=
WiDrMojKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{fBe|czKGh?NH;CWXJFVVORNYTZZ|RrUUN3ME2wMlA2OiEQvF2=MoDVNVU3OTV3MUK=
PC3NELLVWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3S2W|czKGh?NWLqNplDTE2VTx?=MXLJR|UxRTBwMEC5OEDPxE1?M4XaN|E2PjF3NUGy
MDA-MB-231NX3DWZdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NID3WVY4OiCqMnXUSG1UVw>?NV71dmVrUUN3ME2wMlAyOiEQvF2=MnfDNVU3OTV3MUK=
Hs578TMV3DfZRwfG:6aXOgRZN{[Xl?NXPYNGp[PzJiaB?=NGO4VXRFVVORNVLFe2hVT0l3ME2wMlA{KM7:TR?=M{DuN|I1ODF3M{K3
HMECMnviR5l1d3SxeHnjJGF{e2G7Mn3oO|IhcA>?MULEUXNQM4[4c2dKPTB;MT64JO69VQ>?NIXMeoYzPDBzNUOyOy=>
DU145NHfNWYhEgXSxdH;4bYMhSXO|YYm=M4PWbFczKGh?MlPWSG1UVw>?MmfaS2k2OD1yLkG2JO69VQ>?NGHxXlgzPDBzNUOyOy=>
U251NWLOOYdXS3m2b4TvfIlkKEG|c3H5MW[3NkBpMY\EUXNQNHfMZY1IUTVyPUKuPFEh|ryPM1vQcVI1ODF3M{K3
NCI60M4X2R2N6fG:2b4jpZ{BCe3OjeR?=MUe3NkBpM3PvNmROW09?M{OyRmdKPTB;NT63JO69VQ>?MWCyOFAyPTN{Nx?=
MALME-3MMVfDfZRwfG:6aXOgRZN{[Xl?M1fSb|czKGh?Mn\ySG1UVw>?NWjsVoRWT0l3ME22MlYyKM7:TR?=MUiyOFAyPTN{Nx?=
KM12NXzIfWRrS3m2b4TvfIlkKEG|c3H5MlzpO|IhcA>?MX;EUXNQNETJXXlIUTVyPUeuOFQh|ryPMWOyOFAyPTN{Nx?=
SW620NW\sb45sS3m2b4TvfIlkKEG|c3H5MVe3NkBpMYHEUXNQMmfSS2k2OD16LkSzJO69VQ>?MlTJNlQxOTV|Mke=
RXF 393NLNEjC[oFEgXSxdH;4bYMhSXO|YYm=M{H6W|Qh\GG7cx?=MnLjSG1UVw>?Mn\GTWM2OD1yLkCyNVch|ryPMWmyN|I2OzB5NB?=
LXFA 983LMnLMR5l1d3SxeHnjJGF{e2G7MXG0JIRigXN?MnvOSG1UVw>?Mn;OTWM2OD1yLkC1OlUh|ryPNVL0WVQ4OjN{NUOwO|Q>
PRXF DU145NYnHN4hPS3m2b4TvfIlkKEG|c3H5NUPGR4xLPCCmYYnzMYPEUXNQM{TBb2lEPTB;MD6wOlI{KM7:TR?=MWOyN|I2OzB5NB?=
PAXF 1657LMVHDfZRwfG:6aXOgRZN{[Xl?NEHVb2Y1KGSjeYO=NHjxc3NFVVORMkHhTWM2OD1yLkGyNUDPxE1?Ml74NlMzPTNyN{S=
CXF 1103LM4TvbmN6fG:2b4jpZ{BCe3OjeR?=MXW0JIRigXN?M4n3fGROW09?M17kO2lEPTB;ND6zOkDPxE1?MUeyN|I2OzB5NB?=
GXF251LM3fabGN6fG:2b4jpZ{BCe3OjeR?=NIPjWIk1KGSjeYO=NUfqTY42TE2VTx?=MljzTWM2OD1{LkK1JO69VQ>?MVWyN|I2OzB5NB?=
NCI-H23NEfEblJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFzofHE4OiCqNX3YTYl2TE2VTx?=NYi1W|I3UUN3ME2yMlI4KM7:TR?=M4HSNlI{PTJzMEKw
HCT116Ml71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVi3NkBpMXrEUXNQMU\JR|UxRTJwMzFOwG0>NVLWNnpHOjN3MkGwNlA>
MCF7MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXfsfGd6PzJiaB?=MnSzSG1UVw>?NEXtTWpKSzVyPUKuOVch|ryPNVTiWotYOjN3MkGwNlA>
NCI-H460NYfDWmpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIS5R|A4OiCqNVPkemdwTE2VTx?=NGLyeIVKSzVyPUiuPVkh|ryPNF7j[|kzOzV{MUCyNC=>
DLD1NWXyNIpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnHtO|IhcA>?M3vlSWROW09?NHnwWppKSzVyPUSuOkDPxE1?MVuyN|U3Pzl4MB?=
NCI-H661M2HwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1[0flczKGh?NVj1[otSTE2VTx?=M2PrW2lEPTB;Nz64JO69VQ>?MYSyN|U3Pzl4MB?=
A549NFvI[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnPQO|IhcA>?NUnxelFOTE2VTx?=NULhW5lxUUN3ME24MlIh|ryPMmLONlM2Pjd7NkC=
U937MlyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVG3NkBpMnTlSG1UVw>?M2DmWWlEPTB;MUKuNkDPxE1?M2j2SFI{PTZ5OU[w
HEK293NYfjeHp4TnWwY4Tpc44hSXO|YYm=NXPDZWVxOTEEoN88US=>MlXJSG1UVw>?MnLzTY5lfWOnczDibY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIH\1cIwudGWwZ4ToJGhqey22YXfn[YQhVXm2MTDrbY5ie2ViZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyC5aYToJGlEPTBib3[gNE4xPjQQvF2=MlrUNlI4PzB4MUC=
HUVECNWHX[GtMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1zUW|AvOTYEoN88US=>NUXPUmtTPzJiaB?=M3W3VWROW09?MnvsTY5lfWOnczDhcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCrbjDIWXZGSyClbz3jeYx1fXKnZDD3bZRpKH[jc3P1cIFzKHOvb3;0bEBufXOlbHWgZ4VtdHNiYYPz[ZN{\WRiYYOgTY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDheEAxNjF3IIXNMmnENlI5PTN7OUO=
HUVECM{nRW2Z2dmO2aX;uJGF{e2G7NUe3WmJFOTYEoN88US=>MVi3NkBpMom1SG1UVw>?MULJcoR2[2W|IHHueIlidmerb3flcolkKGGldHn2bZR6KGmwIFjVWmVEKGOxLXP1cJR2emWmIIfpeIghfmG|Y4XsZZIhe22xb4ToJI12e2OuZTDj[YxteyCjc4Pld5Nm\CCjczDJcohq[mm2aX;uJI9nKG6ndIfvdosh\m:{bXH0bY9vKGG2IEGuPEB1dyBzNTD1US=>MoPJNlI5PTN7OUO=
Plasmodium falciparumNHTRWItHfW6ldHnvckBCe3OjeR?=NIrheGwyOMLizszNNUexU|lEOTVibXnuM1zkOGROW09?NWnrSnY6UW6qaXLpeJMhWGyjc33v[Il2dSCoYXzjbZBienWvIIDyc4xq\mW{YYTpc44h[nliaX7obYJqfGmwZzD0bIUhTnWwY4Tpc44hd2ZiUH\DSHBMOSCycn;0[YlvKHerdHigTWM2OCCxZjCxMlE4|ryPNVvCPINjOjR3NUCzN|A>
PC3MVzGeY5kfGmxbjDBd5NigQ>?MWCwMlEh|ryPNILlcII2KGh?MV7EUXNQNWO0ZotNUW6qaXLpeJMhcHWvYX6gVGM{KGOnbHygZYRp\XOrb36gZZQhOTByIH7NMXGxPVQ3Ojl5NR?=
DU145NH31e4pHfW6ldHnvckBCe3OjeR?=NY\DXmRDOC5zIN88US=>NWrjNpdjPSCqMo[1SG1UVw>?NHzlZW9KdmirYnn0d{BpfW2jbjDEWVE1PSClZXzsJIFlcGW|aX;uJIF1KDFyMDDuUS=>MlXJNVk1PjJ7N{W=
PC3MVTLbY5ie2ViQYPzZZk>MnLuNE4yKM7:TR?=M3[2dlUhcA>?NX;HNFU4TE2VTx?=MVrJcohq[mm2czDjV5JkKGmwIHj1cYFvKFCFMzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YheGixc4Doc5J6dGG2ZXSgV5JkKFl2MU[gcIV3\WxiYYSgNVAxKG6PMoP6NVk1PjJ7N{W=
DU145NV3FOFVEU2mwYYPlJGF{e2G7NWHsfJJQOC5zIN88US=>MnHTOUBpMUHEUXNQNWX3SWFIUW6qaXLpeJMh[1O{YzDpckBpfW2jbjDEWVE1PSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gdIhwe3Cqb4L5cIF1\WRiU4LjJHk1OTZibHX2[Ywh[XRiMUCwJI5OMUKxPVQ3Ojl5NR?=
PC3NVzpeXc2U2mwYYPlJGF{e2G7NFLIbIgxNjFizszNMWq1JIg>NYHKRZk{TE2VTx?=MWfJcohq[mm2czDjV5JkKGmwIHj1cYFvKFCFMzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YheGixc4Doc5J6dGG2ZXSgSmFMKFl3N{[vXVU4PyCuZY\lcEBifCBzMECgcm0>MoPVNVk1PjJ7N{W=
DU145MV\LbY5ie2ViQYPzZZk>MUOwMlEh|ryPMoTnOUBpMYrEUXNQMo[wTY5pcWKrdIOgZ3Nz[yCrbjDoeY1idiCGVUG0OUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZicHjvd5Bpd3K7bHH0[YQhTkGNIGm1O|YwYTV5NzDs[ZZmdCCjdDCxNFAhdk1?MVqxPVQ3Ojl5NR?=
Huh7MlHCRY51cX[rcnHsJGF{e2G7NGP6XXMzNjVizszNMlP3OEBl[Xm|M{\0WGROW09?M3XyPWlvcGmkaYTzJJZqemGuIIPwdoVi\CCrbjDE[Y5ofWVidnnyeZMucW6oZXP0[YQhcHWvYX6gTJVpPyClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gc4Yhfmm{YXyg[Y53\WyxcHWgdJJwfGWrbjD3bZRpcW5icHXybY52[2ynYYKgdoVocW:wIHH0JFIvPSC3TR?=M3OwWFE4OzZyNke2
C6/36MUPBcpRqfmm{YXygRZN{[Xl?NHvMbY4zNjVizszNMmK5OEBl[Xm|M3;ER2ROW09?NWO5WmdGUW6qaXLpeJMhfmm{YXygd5Bz\WGmIHnuJGRmdme3ZTD2bZJ2ey2rbn\lZ5Rm\CCjc3nhckB1cWencjDtc5NyfWm2bzDDOk8{PiClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gc4Yhfmm{YXyg[Y53\WyxcHWgdJJwfGWrbjD3bZRpcW5icHXybY52[2ynYYKgdoVocW:wIHH0JFIvPSC3TR?=MWmxO|M3ODZ5Nh?=
U937NFLFVZVHfW6ldHnvckBCe3OjeR?=MkfsNUDPxE1?NYnzRpdIOSCqMluySG1UVw>?M2H2U3Jm\HWlZYOgZoF{[WxiVF7GZYxxcGFicnXs[YF{\SCrbjDoeY1idiCXOUO3JINmdGy|NF7qeJgyPzZ6NEC5PS=>
U937M{\CUmZ2dmO2aX;uJGF{e2G7MmXhNUDPxE1?NIXQNngyKGh?NF;E[WdFVVORMYDS[YR2[2W|IFzQV{1qdmS3Y3XkJHRPTmGucHjhJJJmdGWjc3WgbY4hcHWvYX6gWVk{PyClZXzsdy=>M2TEflE4Pjh2MEm5
murine mast cellNGO1TYRHfW6ldHnvckBCe3OjeR?=MWCxJO69VQ>?MnTaNlQhcA>?NXLlTlA4TE2VTx?=MVHJcohq[mm2czDhcpRq\2WwLXnu[JVk\WRiSVy2JJNm[3KndHnvckBqdiCLZ1WgdJJqdWWmIH3veZNmKG2jc4SgZ4VtdHNiYYSgNUB2VQ>?NI[wVoIyPzZ6NEC5PS=>
BV-173NGniSmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVn0O3B7UUN3ME2wMlAxODByMEGwPUDPxE1?NFq2WIhUSU6JRWK=
K-562NHXGflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXPJR|UxRTBwMECwNFAxOjZ4IN88US=>M4LhfHNCVkeHUh?=
BL-70M2TJRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXvJR|UxRTBwMECwNFAxQDJ{IN88US=>MV;TRW5ITVJ?
EM-2Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mn36TWM2OD1yLkCwNFAxOTB6IN88US=>Mny0V2FPT0WU
LAMA-84M4DCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2jyNWlEPTB;MD6wNFAxODN{MTFOwG0>NFGwVXRUSU6JRWK=
MEG-01M3rLfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NX7VRlIxUUN3ME2wMlAxODByOUig{txONHS4ZohUSU6JRWK=
EoL-1-cellM4\sbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEX1fY5KSzVyPUCuNFAxODF|MTFOwG0>NHjLe3hUSU6JRWK=
CTV-1NVu0RY9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIHQVGtKSzVyPUCuNFAxODRyNDFOwG0>M2fzVHNCVkeHUh?=
TE-15MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVHJR|UxRTBwMEC1PFkh|ryPMVTTRW5ITVJ?
NOS-1MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2HXW2lEPTB;MD6wNFYyOyEQvF2=NUXSbZdFW0GQR1XS
D-336MGNEjPdYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3nCfGlEPTB;MD6wNFY{KM7:TR?=NV;ySZNvW0GQR1XS
LB1047-RCCNYHqcJFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnPRTWM2OD1yLkCwPVg6KM7:TR?=Mon0V2FPT0WU
LB996-RCCMVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlTBTWM2OD1yLkCwPVkyKM7:TR?=NEnocpZUSU6JRWK=
SW982M4PUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkXiTWM2OD1yLkCxNVE2KM7:TR?=NVTVV3VkW0GQR1XS
TK10M3fHbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIm5WIhKSzVyPUCuNFEyPzRizszNMn3qV2FPT0WU
A704MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX\JR|UxRTBwMEG0PVEh|ryPM3PZXHNCVkeHUh?=
TE-8NXf6UmFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MX3JR|UxRTBwMEG1O|Yh|ryPNV3mS4tFW0GQR1XS
DOHH-2MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3jiXGlEPTB;MD6wNVcyQSEQvF2=NGTpVopUSU6JRWK=
HOP-62NVXWSJV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1TKSGlEPTB;MD6wNVg{PCEQvF2=NUT1S45FW0GQR1XS
TE-12MofWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MWPJR|UxRTBwMEG4OlEh|ryPMWLTRW5ITVJ?
KGNM{LyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnK0TWM2OD1yLkCxPVQzKM7:TR?=Mn7aV2FPT0WU
NCI-H1648MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGjFPJlKSzVyPUCuNFIxOTFizszNMl24V2FPT0WU
OS-RC-2MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2LuOmlEPTB;MD6wNlA{KM7:TR?=M3v6SHNCVkeHUh?=
GB-1NIHjPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NIXXOJZKSzVyPUCuNFIyPTdizszNNEDDWXpUSU6JRWK=
RXF393M2T1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXPObmNPUUN3ME2wMlAzOzV5IN88US=>M33KTnNCVkeHUh?=
LC-2-adNILLcGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MWLJR|UxRTBwMEK1PFYh|ryPNIrQT|JUSU6JRWK=
KS-1NX;ndFRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{LIeGlEPTB;MD6wNlc{KM7:TR?=MXLTRW5ITVJ?
ETK-1M4jle2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXPJR|UxRTBwMEK4N|Ih|ryPNEXweINUSU6JRWK=
SW954NWfHTXE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVTJR|UxRTBwMEK5Nlch|ryPM3jaVHNCVkeHUh?=
BeckerNFnHPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXXJR|UxRTBwMEOwNFMh|ryPMnHIV2FPT0WU
MZ1-PCNGHNb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWHiW3dHUUN3ME2wMlA{OTF7IN88US=>MYHTRW5ITVJ?
ES6MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIPufGJKSzVyPUCuNFMyQTNizszNNVLUNoFlW0GQR1XS
KURAMOCHINXPocpFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NGXpeFZKSzVyPUCuNFM1QDdizszNMl35V2FPT0WU
CGTH-W-1NVm5dWNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUfuW4pkUUN3ME2wMlA{PTR6IN88US=>MXnTRW5ITVJ?
VA-ES-BJNF3YenVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NILwXmNKSzVyPUCuNFM6ODJizszNNF:z[mlUSU6JRWK=
LXF-289M3S5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M33tWWlEPTB;MD6wN|k2PiEQvF2=NY\TcGkzW0GQR1XS
MPP-89NV\BVlhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIi4OJpKSzVyPUCuNFQxPDlizszNMlr3V2FPT0WU
SW872NUXXT49WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mn[yTWM2OD1yLkC0NVYyKM7:TR?=MUnTRW5ITVJ?
SNB75MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVmzRoJnUUN3ME2wMlA1PDN3IN88US=>MmXvV2FPT0WU
PSN1M2DYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkfnTWM2OD1yLkC0OFc1KM7:TR?=M4XWXHNCVkeHUh?=
LB831-BLCM{nVUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXTJR|UxRTBwMES2NFkh|ryPNFXFWGdUSU6JRWK=
MFH-inoM3HoWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkPITWM2OD1yLkC0O|I1KM7:TR?=MlLuV2FPT0WU
TGBC24TKBNULJ[5N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M171PGlEPTB;MD6wOFc3OSEQvF2=NXGwUWJsW0GQR1XS
A388M1e4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVf6TGR{UUN3ME2wMlA2ODl3IN88US=>MVLTRW5ITVJ?
BB30-HNCNYPMSGppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NX:4eJA5UUN3ME2wMlA2PDN5IN88US=>NVz1WYdxW0GQR1XS
GI-ME-NMmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlnETWM2OD1yLkC2NVE5KM7:TR?=MX;TRW5ITVJ?
TGBC1TKBM3LWbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXPWVYxbUUN3ME2wMlA3OTZ2IN88US=>MYnTRW5ITVJ?
TE-10M{PP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXTPcZh6UUN3ME2wMlA3OzV5IN88US=>NF3vbWxUSU6JRWK=
A498NWPOTFlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1L5SmlEPTB;MD6wO|I5PCEQvF2=MmfXV2FPT0WU
TE-11NWXFNGpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NU\6UI44UUN3ME2wMlA4QDV6IN88US=>M2P1cHNCVkeHUh?=
BB65-RCCMUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NV:yfZl3UUN3ME2wMlA5OjJ5IN88US=>M{jJfnNCVkeHUh?=
C2BBe1NWjIc5k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NYnhWI1OUUN3ME2wMlA5OzB6IN88US=>NVLRR4duW0GQR1XS
NCI-H747NWLoZ3RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoPHTWM2OD1yLkC4N|YzKM7:TR?=MYTTRW5ITVJ?
IST-MES1NHLKXWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHHhToRKSzVyPUCuNFg2PTJizszNMXPTRW5ITVJ?
KALS-1M1XFemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXWyVFRNUUN3ME2wMlA6PDlizszNMnSzV2FPT0WU
GCIYM2D3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MoDyTWM2OD1yLkC5OlU3KM7:TR?=NUHEWZV6W0GQR1XS
RL95-2M3;5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXPDdFFSUUN3ME2wMlExOzhizszNMlrGV2FPT0WU
TE-1MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFrYTlZKSzVyPUCuNVA2PCEQvF2=MlXMV2FPT0WU
NCI-H1355NGLQZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYLjO4JFUUN3ME2wMlEyODJ6IN88US=>NXXHNHN4W0GQR1XS
SW962MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlfsTWM2OD1yLkGxNlkzKM7:TR?=M4\ITHNCVkeHUh?=
KLEM2DTfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmDDTWM2OD1yLkGxN|E4KM7:TR?=NUHWcI9VW0GQR1XS
MC116NUPFTZhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnrqTWM2OD1yLkGxOFEh|ryPMX;TRW5ITVJ?
NMC-G1NXfq[pZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWrJR|UxRTBwMUG2NFYh|ryPM4DkNHNCVkeHUh?=
KU812NHLwUIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3O1fmlEPTB;MD6xNVg5OyEQvF2=M4nmWnNCVkeHUh?=
COLO-829M37YRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUnafZFkUUN3ME2wMlEzOjF|IN88US=>MonZV2FPT0WU
NTERA-S-cl-D1NFvHTm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXrJR|UxRTBwMUKyPFMh|ryPM4jaWXNCVkeHUh?=
IST-MEL1NVPtV4dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIPnZ3lKSzVyPUCuNVM1PSEQvF2=M1TsWHNCVkeHUh?=
MLMANU\POIpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXnHW2h1UUN3ME2wMlE1ODN{IN88US=>NYXNXXViW0GQR1XS
LS-123NYP2VoJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVTJR|UxRTBwMUSwOlQh|ryPNFXtfZFUSU6JRWK=
LB2518-MELMnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIXDcVJKSzVyPUCuNVQyPjJizszNM2Kzd3NCVkeHUh?=
NB69MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWS0dm45UUN3ME2wMlE1PDN4IN88US=>NYfYboF5W0GQR1XS
8-MG-BAMYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{O3bmlEPTB;MD6xOVQ2QCEQvF2=Mn7XV2FPT0WU
K5MnzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NY\wZ2NQUUN3ME2wMlE3PDh7IN88US=>MkXRV2FPT0WU
KINGS-1M3LiSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYPJR|UxRTBwMU[2OlYh|ryPMX7TRW5ITVJ?
SF268M1HEc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGO1dXVKSzVyPUCuNVc1ODRizszNMXvTRW5ITVJ?
PF-382M1vSRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mkm0TWM2OD1yLkG3Olc5KM7:TR?=MVHTRW5ITVJ?
SH-4NUj4SFFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NU\PNIRsUUN3ME2wMlE5PDF|IN88US=>MYnTRW5ITVJ?
NALM-6M2\xR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NX;lZXlxUUN3ME2wMlE6Ojl3IN88US=>M2rNS3NCVkeHUh?=
CP66-MELMWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3Hk[WlEPTB;MD6xPVU{OSEQvF2=MWTTRW5ITVJ?
697M2H2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWnJR|UxRTBwMUm5PFch|ryPM17WcXNCVkeHUh?=
CP67-MELMUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3HLUWlEPTB;MD6yNFQ5QCEQvF2=MUnTRW5ITVJ?
DSH1MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mni1TWM2OD1yLkK0NFAyKM7:TR?=M4HOWHNCVkeHUh?=
HCE-4NXntN2xST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHfpWIJKSzVyPUCuNlY1OzlizszNNVPIeFRYW0GQR1XS
MZ2-MELM3j3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4\DfmlEPTB;MD6yPFU{PyEQvF2=MVPTRW5ITVJ?
BL-41Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUjVSIpbUUN3ME2wMlI6OTJ|IN88US=>MoLsV2FPT0WU
HUTU-80MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnrQTWM2OD1yLkOxOFIh|ryPNYPiU5lVW0GQR1XS
LOXIMVINEfqZWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3zGTWlEPTB;MD6zNVUxOyEQvF2=Mkj6V2FPT0WU
no-10M3XjZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXjBUGQ3UUN3ME2wMlMyQTNzIN88US=>M2PYOnNCVkeHUh?=
KARPAS-422NFe5dWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmjhTWM2OD1yLkOzPVk4KM7:TR?=Ml\HV2FPT0WU
SW684M4npbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVrJR|UxRTBwM{S5PEDPxE1?NIP1[ZpUSU6JRWK=
SF126MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MoXiTWM2OD1yLkO1OFEh|ryPMn36V2FPT0WU
D-263MGNXr3TZNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MojCTWM2OD1yLkO2NlI1KM7:TR?=NITudFNUSU6JRWK=
OVCAR-4NFnyNpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MYjJR|UxRTBwM{e0N|Mh|ryPMoPKV2FPT0WU
BB49-HNCNIPHcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXmwd2JmUUN3ME2wMlM5PTl7IN88US=>MlfyV2FPT0WU
ONS-76NIjyT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MWPJR|UxRTBwNEK5OVEh|ryPNXuxOoE{W0GQR1XS
MZ7-melNW\mWXE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIXreHRKSzVyPUCuOFc6OTFizszNNXG0WmFpW0GQR1XS
RCC10RGBMVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MULJR|UxRTBwNEmxNUDPxE1?NXvMXHE6W0GQR1XS
BOKUNIDk[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlHRTWM2OD1yLkS5NVM{KM7:TR?=MoDSV2FPT0WU
no-11M{LSSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4KwUGlEPTB;MD61NFIzQCEQvF2=NYri[4hvW0GQR1XS
IST-SL2MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX7JR|UxRTBwNUCzNFIh|ryPNXTNVnBoW0GQR1XS
RKOMVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWTJR|UxRTBwNUK5OlYh|ryPMVfTRW5ITVJ?
HT-144M4TnOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mn72TWM2OD1yLkWzOlA6KM7:TR?=M4PaUHNCVkeHUh?=
NCI-H446NYj5NVdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFPQT3ZKSzVyPUCuOlI4PiEQvF2=NVOwc5EzW0GQR1XS
QIMR-WILMn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MoK0TWM2OD1yLkewOlI6KM7:TR?=NIHXc5NUSU6JRWK=
MHH-PREB-1NGDZd|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXXJR|UxRTBwN{S0Olkh|ryPNX76cXhSW0GQR1XS
EW-16M1L0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkPiTWM2OD1yLke2NVc5KM7:TR?=MUjTRW5ITVJ?
EW-24NGTUbHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mk[zTWM2OD1yLke4NVY2KM7:TR?=MWrTRW5ITVJ?
LB373-MEL-DNUKxSVdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVnwSWdLUUN3ME2wMlgzPTB6IN88US=>NGi5RnBUSU6JRWK=
TE-9M4rRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYfXOXVKUUN3ME2wMlg4PTN{IN88US=>M4T5b3NCVkeHUh?=
A3-KAWMVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWfY[VdsUUN3ME2wMlk5PDV{IN88US=>Mm\pV2FPT0WU
A101DNVGxPI0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXP1OWt2UUN3ME2xMlA{ODR|IN88US=>NXzCVnA1W0GQR1XS
OCUB-MNVvxb|A1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{LkVWlEPTB;MT6wOFQyOiEQvF2=M1O5S3NCVkeHUh?=
ES4MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NF;sTWFKSzVyPUGuNFUyPDVizszNNEHnUnFUSU6JRWK=
TE-6MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MonITWM2OD1zLkKxNlI3KM7:TR?=M1q3[3NCVkeHUh?=
D-502MGMWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3fiU2lEPTB;MT6yN|M4PiEQvF2=MmnPV2FPT0WU
KNS-42NIHneFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NE\MXIhKSzVyPUGuNlQ1OTJizszNMnnKV2FPT0WU
SNU-C2BNFLEflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmjSTWM2OD1zLkOwOVg6KM7:TR?=NXjpTpQ5W0GQR1XS
NCI-H1838MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXr6b5BxUUN3ME2xMlMxPzN|IN88US=>M{HDWXNCVkeHUh?=
NKM-1NUC0ZmRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2[wZmlEPTB;MT6zNFg2QSEQvF2=NWTIcXlzW0GQR1XS
GI-1M13OT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MULJR|UxRTFwM{[yNkDPxE1?MmrqV2FPT0WU
NB5MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkTsTWM2OD1zLkO5PFI4KM7:TR?=Mo\IV2FPT0WU
CAS-1Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmnsTWM2OD1zLkSwPVkzKM7:TR?=MU\TRW5ITVJ?
HCE-TM1LGeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUjFOlZQUUN3ME2xMlU3PzF2IN88US=>MmCyV2FPT0WU
SBC-1MnHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4e4SWlEPTB;MT61O|k5PCEQvF2=MX3TRW5ITVJ?
JiyoyeP-2003MlW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2KyW2lEPTB;MT63N|Q3PiEQvF2=MnezV2FPT0WU
TE-5NHLUTZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF\mPYNKSzVyPUGuO|kyOzlizszNMmTKV2FPT0WU
CANNV\MOopUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmjNTWM2OD1zLkiyNlUzKM7:TR?=M3vo[nNCVkeHUh?=
SK-UT-1NF22PHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{P3N2lEPTB;Mj6xOlY6OyEQvF2=NWP0TJhlW0GQR1XS
JVM-2M2TVOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEXYblBKSzVyPUKuN|YzQDRizszNMX;TRW5ITVJ?
LB771-HNCMYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFX1PJhKSzVyPUKuOVc2PTFizszNM{HtTXNCVkeHUh?=
NCCITNHjY[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2\p[GlEPTB;Mj64OlYyPiEQvF2=MYHTRW5ITVJ?
NCI-H2126NYXjdW5NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnvZTWM2OD1{Lki3OVUzKM7:TR?=NXXzd2c3W0GQR1XS
Calu-6MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmThTWM2OD1|LkC1O|QyKM7:TR?=M4Ty[3NCVkeHUh?=
SK-LMS-1NGDTd4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M17mN2lEPTB;Mz6xNVg5PiEQvF2=M3TFU3NCVkeHUh?=
ARH-77M2frXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NH;ERoNKSzVyPUOuOFY6OTVizszNNIK3SHpUSU6JRWK=
NB17M1zneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlmyTWM2OD1|Lk[zPFQ4KM7:TR?=NHLjXnpUSU6JRWK=
A253MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYTJR|UxRTNwN{OyOFYh|ryPMX;TRW5ITVJ?
OPM-2NHrKTHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MojKTWM2OD12LkK3Olg2KM7:TR?=NEHIdWlUSU6JRWK=
MV-4-11MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MoX1TWM2OD12LkO2OFU1KM7:TR?=M4POeXNCVkeHUh?=
SRM36zb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHjkU4pKSzVyPUSuOFk6PTRizszNNFPaRVhUSU6JRWK=
KG-1M3XL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHvuN2JKSzVyPUSuOlA5PDVizszNNGHETI1USU6JRWK=
OCI-AML2MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1XTVGlEPTB;NT64OlE2PCEQvF2=MVjTRW5ITVJ?
D-247MGMWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXHWTJdpUUN3ME22MlEzPTF7IN88US=>MmL3V2FPT0WU
DJM-1M{TXUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmW3TWM2OD14LkS4OVU5KM7:TR?=NH[xOmVUSU6JRWK=
RPMI-6666NF;MbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1y0N2lEPTB;Nz6yO|A3PyEQvF2=NGLVSpFUSU6JRWK=
KARPAS-45M3PGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mlv2TWM2OD15LkWxOlcyKM7:TR?=NFTueWRUSU6JRWK=
LP-1NGDvNoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MWPJR|UxRTdwNUS3PFIh|ryPMorTV2FPT0WU
RS4-11MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mn\iTWM2OD15Lk[1O|g4KM7:TR?=NVvrcYZrW0GQR1XS
DU-4475NWTLWpNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFz6bnNKSzVyPUiuNlE3PTJizszNNXTBfG5YW0GQR1XS
MONO-MAC-6NXvmelBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoLqTWM2OD16LkK3NFY3KM7:TR?=NWm4UWVsW0GQR1XS
NCI-SNU-16MmCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3y5O2lEPTB;OD61OlEzQCEQvF2=NHHITJRUSU6JRWK=
SJSA-1NXHMV4ZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4T4[GlEPTB;OD63NlgxPSEQvF2=M3nhOXNCVkeHUh?=
MMAC-SFNYnmb|MzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MV\JR|UxRThwN{mzNFch|ryPNX3XSZBsW0GQR1XS
SK-NEP-1NGfhN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MorzTWM2OD16Lki5NVU2KM7:TR?=NEPJZXlUSU6JRWK=
J-RT3-T3-5MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Ml64TWM2OD16Lkm2OVI6KM7:TR?=MXHTRW5ITVJ?
SKM-1MoOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWXmeINIUUN3ME25MlAyPzN2IN88US=>MlrnV2FPT0WU
LB2241-RCCNVjCSlByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MlvkTWM2OD17LkCyNFEzKM7:TR?=MnnlV2FPT0WU
SIG-M5MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4TUTGlEPTB;OT6wNlQ6OyEQvF2=MUXTRW5ITVJ?
EVSA-TNITOPYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkPhTWM2OD17LkK3O|k{KM7:TR?=NIi5[m1USU6JRWK=
GT3TKBNInF[JBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1jaSGlEPTB;OT6zOVU1PiEQvF2=M1nrW3NCVkeHUh?=
NB6M4TR[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1fm[2lEPTB;OT65NlI2QSEQvF2=MnzLV2FPT0WU
EHEBNFz1OmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF7SUndKSzVyPUGwMlA3PTZizszNNFPkXI5USU6JRWK=
HELNYHVVoxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MlHQTWM2OD1zMD60O|c3KM7:TR?=NEP4W2ZUSU6JRWK=
ALL-POMVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXXJR|UxRTFyLke5N|gh|ryPMojNV2FPT0WU
TGWNFzt[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnX6TWM2OD1zMT6yPFI5KM7:TR?=MoDzV2FPT0WU
BC-3MmLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHm1Zo9KSzVyPUGyMlEyOzhizszNNWPvO3FnW0GQR1XS
IA-LMMoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NX3JNmJMUUN3ME2xNk41PDR3IN88US=>MkXJV2FPT0WU
UACC-257M37icWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVLJR|UxRTF{LkmxPVgh|ryPNX[4cYNmW0GQR1XS
KP-N-YSNHK0fWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MWHJR|UxRTF{LkmyPFMh|ryPM3v3W3NCVkeHUh?=
RajiMn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIjHV2xKSzVyPUGzMlc1QTdizszNNVzWUIdwW0GQR1XS
SF539NUfUNYlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFLDcohKSzVyPUGzMlg2PTdizszNNUOxfmJtW0GQR1XS
DMS-153NGLv[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4\0W2lEPTB;MUSuNFAzQCEQvF2=M2PzcHNCVkeHUh?=
L-540M4DOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3r1OWlEPTB;MUWuNFY4OiEQvF2=NIjwb5NUSU6JRWK=
MN-60MlHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MX7JR|UxRTF3LkG5O|kh|ryPNYPHR5k4W0GQR1XS
RPMI-8866M1r3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWfJR|UxRTF5LkS0OVQh|ryPM4jDW3NCVkeHUh?=
NCI-H510AM{fpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEjZVGJKSzVyPUG5MlM6PzNizszNMUDTRW5ITVJ?
NB13M1HBbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4HGNGlEPTB;MUmuOFg4PyEQvF2=M2ewPHNCVkeHUh?=
HAL-01NUnjeFZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NEPLdIdKSzVyPUG5Mlc2PDNizszNM{DwRXNCVkeHUh?=
NCI-H720NXfJfppJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{j1SWlEPTB;MkCuNlc{OyEQvF2=M1z4[HNCVkeHUh?=
REHNFHhXHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHfxdXRKSzVyPUKwMlY{PTdizszNMUXTRW5ITVJ?
KNS-81-FDM4nnRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUfJR|UxRTJ|LkG0OkDPxE1?MoGxV2FPT0WU
HC-1M1qwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUTJR|UxRTJ2LkW1OVEh|ryPMkLGV2FPT0WU
NCI-H2141MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NGLT[YtKSzVyPUK0Mlc4PTRizszNNXHyPXlGW0GQR1XS
MOLT-4MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWLufWNiUUN3ME2yOk43PzV|IN88US=>M4jDd3NCVkeHUh?=
OMC-1MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NX;WRYdNUUN3ME2yO{4yPDJ{IN88US=>NX3UdVY3W0GQR1XS
LC-1FMXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGnoUXlKSzVyPUK3MlMzPDVizszNMWDTRW5ITVJ?
NCI-H1304NWSzeI9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1u1VGlEPTB;MkiuNVYzQCEQvF2=NV;0V5pbW0GQR1XS
BC-1NX3r[YhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2\UPGlEPTB;MkiuOlUyKM7:TR?=MlPrV2FPT0WU
NCI-H64NHXGSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4DQVmlEPTB;MkmuOlI2OyEQvF2=MV;TRW5ITVJ?
MOLT-16MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mn3QTWM2OD1{OT62NlkzKM7:TR?=MWfTRW5ITVJ?
U-87-MGNFvpb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NIi3fXlKSzVyPUOwMlc3PiEQvF2=M{fHSnNCVkeHUh?=
GAKM{D5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkDZTWM2OD1|MT6yOlg3KM7:TR?=M3HE[XNCVkeHUh?=
ES8MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NILwVmRKSzVyPUOyMlEzPTJizszNNW\OOol4W0GQR1XS
HCC1599M3zGcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHOydJJKSzVyPUOyMlM{OjVizszNM4P5SHNCVkeHUh?=
EB-3M3LrV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MV;JR|UxRTN2LkOxNVch|ryPM{fqc3NCVkeHUh?=
HCC1187NIjWV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGPudIpKSzVyPUO1MlgxPTJizszNM2XiNHNCVkeHUh?=
SK-PN-DWMVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MojITWM2OD1|Nj6xPVQ{KM7:TR?=MoHOV2FPT0WU
JVM-3NUDzcWFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnfuTWM2OD1|Nz6yN|M5KM7:TR?=NYHnblZwW0GQR1XS
HCC2157Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHO1NoZKSzVyPUO3Mlk6PDZizszNNEPTN4RUSU6JRWK=
A4-FukNXP3U2xXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVnEbYpRUUN3ME2zPE4yODB7IN88US=>NH;4R2pUSU6JRWK=
COR-L279NGHacm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlWxTWM2OD12MD6yPFUyKM7:TR?=MmLpV2FPT0WU
DELMWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3;KPGlEPTB;NEGuPVA5PiEQvF2=MXnTRW5ITVJ?
NCI-H1395MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUToXmhXUUN3ME20Nk4xOTZ|IN88US=>NHXyN2lUSU6JRWK=
MHH-NB-11MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2fKdmlEPTB;NEOuNFgyQCEQvF2=NVnyOmJyW0GQR1XS
NCI-H2107NFHkSFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmjhTWM2OD12Mz60PFQ3KM7:TR?=MlvLV2FPT0WU
NEC8MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NF3ZU4NKSzVyPUS0MlM{PiEQvF2=NG\ISVBUSU6JRWK=
COLO-684NIHaOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M37ETmlEPTB;NE[uNlI2QCEQvF2=NWHFRoNoW0GQR1XS
LS-411NNX;Lb4ZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHzVeZBKSzVyPUS4MlQ4PDhizszNMYPTRW5ITVJ?

... Click to View More Cell Line Experimental Data

In vivo Dasatinib reverses splenomegaly in LMP2A/MYC double transgenic mice. Dasatinib specifically prevents colony formation by LMP2A expressing bone marrow B cells and decreased spleen size in the TgE mice. Spleen mass is significantly decreased among Dasatinib treated Tg6/λ-MYC mice when compared to the control group. Dasatinib inhibits lymphadenopathy in LMP2A/MYC double transgenic mice. Dasatinib reverses splenomegaly in Rag1KO mice engrafted with tumor cells from LMP2A/MYC double transgenic mice. Dasatinib therapy inhibits Lyn phosphorylation in B lymphocyte tumors expressing LMP2A. [3]
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

Kinase autophosphorylation assays Kinase assays using wild-type and mutant glutathione S-transferase (GST)-Abl fusion proteins (c-Abl amino acids 220-498) are done. GST-Abl fusion proteins are released from glutathione-Sepharose beads before use; the concentration of ATP is 5 μM. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase. After 1-hour incubation at 30 °C, LAR phosphatase is inactivated by addition of sodium vanadate (1 mM). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase is routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The Dasatinib concentration range is extended to 1,000 nM for mutant T315I. These same inhibitor concentrations are used for the in vitro peptide substrate phosphorylation assays. The three inhibitors are tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase.

Cell Assay:

[1]

Cell lines Ba/F3 cell lines
Concentrations ~32 nM
Incubation Time 72 hours
Method

Ba/F3 cell lines are seeded in triplicate and incubated with escalating concentrations of Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges are 0 nM to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 200 nM for mutant T315I.

Animal Study:

[3]

Animal Models EμLMP2A (TgE and Tg6 strains), MYC (λ-MYC), and LMP2A/λ-MYC double transgenic mice (Tg6/λ-MYC)
Formulation DMSO
Dosages 30 mg/kg
Administration Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] O'Hare T, et al. Cancer Res. 2005, 65(11), 4500-4505.

[2] Shah NP, et al. Blood, 2006, 108(1), 286-291.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02709083 Not yet recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University December 2016 Phase 2
NCT02815059 Not yet recruiting Acute Lymphoblastic Leukemia University of Utah|Janssen, LP August 2016 Phase 1
NCT02819804 Not yet recruiting B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblast  ...more B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia|Refractory Childhood Acute Lymphoblastic Leukemia Northwestern University|National Cancer Institute (NCI) July 2016 Phase 1
NCT02744768 Not yet recruiting Acute Lymphoblastic Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto June 2016 Phase 2
NCT02776878 Recruiting Gastrointestinal Stromal Tumor Beijing Cancer Hospital May 2016 --

view more

Chemical Information

Download Dasatinib SDF
Molecular Weight (MW) 488.01
Formula

C22H26ClN7O2S

CAS No. 302962-49-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms BMS-354825
Solubility (25°C) * In vitro DMSO 98 mg/mL (200.81 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide

Customer Product Validation(10)


Click to enlarge
Rating
Source Cell Res 2011 21, 1080-1087. Dasatinib purchased from Selleck
Method Microangiography
Cell Lines embryos
Concentrations 30 μM
Incubation Time
Results MEK1/2 may cooperate with VEGFR to regulate blood vessel lumen diameter. We examined this hypothesis by combining VEGFR inhibitor Sunitinib and MEK1/2 inhibitor U0126. Indeed, U0126 (10 µM) combined with Sunitinib (20 µM) resulted in a reduction of vessel lumen size (Figure F), whereas individually they did not. Combined treatment of another MAP kinase signaling pathway inhibitor Dasatinib (20 µM) with Sunitinib (20 µM) produced a similar phenotype as PP1, whereas each individual inhibitor did not result in any vessel shrinkage even at much higher concentrations ( Figure C).Since there are three major VEGF receptors, it is desirable to determine which receptor is involved in combinatory action with MEK1/2. To address this issue, additional highly selective VEGFR inhibitors PTK787 and ZM323881 were tested. Both of these inhibitors (PTK787 or ZM323881), when individually combined with Dasatinib or U0126, induced a reduction of vessel lumen size (Figure D, E, G, and H).

Click to enlarge
Rating
Source Clin Cancer Res 2011 17, 762-770. Dasatinib purchased from Selleck
Method Assessment of cell viability and apoptosis
Cell Lines B-CLL patient leukemic cells
Concentrations 2-10 μM
Incubation Time 48 h
Results The Dasatinib+Nutlin-3 combination promotes synergistic cytotoxicity in primary CLL cells as well as in p53 wild-type and p53 deleted/ mutated leukemic cell lines.

Click to enlarge
Rating
Source Clin Cancer Res 2011 17, 762-770. Dasatinib purchased from Selleck
Method Western blot
Cell Lines Leukemic cell lines
Concentrations 10 μM
Incubation Time 24 h
Results Dasatinib marginally affected both the basal levels of p53 and the accumulation of p53 induced by Nutlin-3 in the p53 wild -type cells (Fig. A).Interestingly, however, levels of both MDM2 and p21 proteins, 2 of the best characterized transcriptional targets of p53, weres significantly (P < 0.05) decreased in cells treated with Dasatinib+ Nutlin-3 with respect to cells treated with Nutlin-3 alone (Fig. B).

Click to enlarge
Rating
Source Clin Cancer Res 2011 17, 762-770. Dasatinib purchased from Selleck
Method Phospho-kinase array analysis
Cell Lines EHEB cell lines/BJAB cell lines
Concentrations 10 μM
Incubation Time 16 h
Results Although Nutlin-3 had no effects on these pathways, Dasatinib alone as well as Dasatinib+Nutlin-3 markedly inhibited the basal phosphorylation of ERK1/2, p38/MAPK, and Akt . Of interest, the combination of Dasatinib+Nutlin-3 selectively enhanced (P < 0.05) the inhibition of Akt phosphorylation with respect to Dasatinib alone, as validated by Western blot analysis.

Click to enlarge
Rating
Source Biochem Pharmacol 2011 82, 1457-1466. Dasatinib purchased from Selleck
Method MTT assay
Cell Lines MOLM-13 cells, HL-60 cells
Concentrations 1-15 μM
Incubation Time 24-72 h
Results Dasatinib and other TKI decreased the viability of the two myeloid cell lines in a dose- and time-dependent manner. Nevertheless, the anti-leukemic efficacy of Dasatinib and other TKI varied considerably in both cell lines.

Click to enlarge
Rating
Source Biochem Pharmacol 2011 82, 1457-1466. Dasatinib purchased from Selleck
Method Evaluation of differentiation
Cell Lines MOLM-13 cells, HL-60 cells
Concentrations 5 μM
Incubation Time
Results In a first series of experiments, we assessed four signs of morphological differentiation, May-Gruenwald-Giemsa staining of MOLM-13 cells demonstrated that dasatinib induced a dose-dependent decrease in cytoplasmic basophilia and in the nucleo-cytoplasmic ratio. Dasatinib also led to the appearance of dented nuclei and cytoplasmic granulation( Fig.A and B).In HL-60 cells,dasatinib(5 μM) once more exhibited the highest differentiation-inducing capacity. Thus dasatinib diminished basophilia of the cytoplasm concomitantly with the nucleo-cytoplasmic ratio, and induced the appearance of nuclear lobulation and cytoplasmic granules(Fig. G). Next, we determined the degree of CD11b expression, a marker indicating myeloid differentiation, in TKI-treated MOLM-13 dasatinib exhibited the most pronounced capacity to increase CD11b surface expression( Fig. C and D).To corroborate the TKI-driven differentiation, we quantified the enzymatic activity of alkaline phosphatase by means of the NBT-reduction assay after an incubation period of 6 days in MOLM-13 cells.,Once again, the NBT-reductive activity was highest in cells treated with dasatinib, which was as active as the positive control, ATRA( Fig. E and F)

Click to enlarge
Rating
Source Invest New Drugs 2010 30, 417-422. Dasatinib purchased from Selleck
Method Assessment of cell viability
Cell Lines leukemic cells
Concentrations 10 μM
Incubation Time 24/48 h
Results Dasatinib dose-dependently reduced cell viability in all leukemic cell lines, with variable efficacy irrespect ively of the p53 status. In particular, when used at 10 μM, Dasatinib induced a progressive decrease of the total number of viable cells ranging from approximately 30% (JVM-2 and MEC-2) to 50% (EHEB and BJAB) after 48 h of treat ment (Fig.a). In order to investigate whet her the decreased leukemic cell viability was mainly due to either cytotoxic or cytostatic activity, we have analyzed the effects of Dasatinib on apoptosis,As shown in Fig. b, exposure to Dasatinib induced a significant (p < 0.05) increase of apoptosis in all leukemic cell lines, as evaluated by Annexin-V/PI staining at 48 h of treatment.

Click to enlarge
Rating
Source Invest New Drugs 2010 30, 417-422. Dasatinib purchased from Selleck
Method phospho-kinase array analysis
Cell Lines EHEB (p53wt) cell lines, BJAB (p53mut) B cell lines
Concentrations
Incubation Time 24 h
Results As shown in Fig. a , the most evident effects of Dasatinib in both cell models were represented by a significant down-regulation of the phosphorylation levels of p38 MAPK, ERK1/2 and CREB. In addition, densitometric analysis of the phospho-kinase array demonstrated that Dasatinib also inhibited the phosphorylation levels of several STAT family members (STAT1, STAT2, STAT3, STAT5a/b and STAT6), the most evident effect in both p53 wild-type (EHEB) and p53 mutated (BJAB) cell lines being on STAT2, STAT3 and STAT6 (Fig. b)

Click to enlarge
Rating
Source Invest New Drugs 2010 30, 417-422. Dasatinib purchased from Selleck
Method Western blot
Cell Lines p53wild-type(EHEB, JVM-2) cell lines, p53mutated(MEC-2, BJAB) cell lines
Concentrations 10 μM
Incubation Time 24 h
Results "Upon exposure to Dasatinib, a decrease of phosphorylated proteins was confirmed by Western blot analys is in all cell lines investigated without significant differences between p53wild-type and p53mutated cell lines.

Click to enlarge
Rating
Source Dr. Thomas Kruwel of Fraunhofer-Institute for Toxicology and Experimental Medicine-Dasatinib (BMS-354825) purchased from Selleck. Dasatinib purchased from Selleck
Method Cell vability assays
Cell Lines A2C12, Beta D5, Gamma A3, Gamma D12, A549, CaCo2, HepG2 cell lines
Concentrations 0.001-1000 nM
Incubation Time 24/96 h
Results

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Src Products

  • Dasatinib Monohydrate

    Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

  • SU6656

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • PX-478 2HCl

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Saracatinib (AZD0530)

    Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.

    Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

  • Bosutinib (SKI-606)

    Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.

  • KX2-391

    KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.

  • PP1

    PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • PP2

    PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.

  • WH-4-023

    WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50 of 2 nM and 6 nM in cell-free assays, respectively.

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

Recently Viewed Items

Tags: buy Dasatinib | Dasatinib ic50 | Dasatinib price | Dasatinib cost | Dasatinib solubility dmso | Dasatinib purchase | Dasatinib manufacturer | Dasatinib research buy | Dasatinib order | Dasatinib mouse | Dasatinib chemical structure | Dasatinib mw | Dasatinib molecular weight | Dasatinib datasheet | Dasatinib supplier | Dasatinib in vitro | Dasatinib cell line | Dasatinib concentration | Dasatinib nmr
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us