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

Product Use Citation(61)

Customer Product Validation(10)

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
M07ep210NYnIT5hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4G4OlczKGh?NHq3U3BFVVORMXnJR|UxRTBwMECwNFch|ryPNHHiTXQyPzl3NkC4NC=>
K562NGHTSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NULLcXVIPzJiaB?=NFjL[GVFVVORNVHwRZBNUUN3ME2wMlAxOSEQvF2=MX[xO|k2PjB6MB?=
M07eNVPLPIlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHL6cGM4OiCqM2TMVGROW09?MVvJR|UxRTBwMECxNkDPxE1?M4\SVVE4QTV4MEiw
ALL3M2DlfWN6fG:2b4jpZ{BCe3OjeR?=NY\IV25JOC5zzszNMUC3NkBpMlq1SG1UVw>?NYrvRoYyUUN3ME2wMlAxODRizszNMVWxPVg5QTV2MB?=
CMLNEfV[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NG[0UlMzOCCvaX6=NWjqN5c{TE2VTx?=Mkn0TWM2OD1yLkCwNUDPxE1?MXmxPVIyQTBzNh?=
BA/F3MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4\2W|czKGh?NFXT[YZFVVORNXu5TmpXUUN3ME22MlU5QSEQvF2=MVeyN|A5QDZ2NB?=
BA/F3MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEfoUW44OiCqM13JbGROW09?MkDmTY5lfWOnczDhcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDL1[zJINmdGy|IHX4dJJme3OrbnegRoNzNUGkbDDNN|UyXCCvdYThcpQhf2m2aDDJR|UxKG:oIECuNFAxQDQQvF2=NX:xcoJyOjNyOEi2OFQ>
BA/F3NWmyV5VrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUC3NkBpMo\OSG1UVw>?MXvJcoR2[2W|IHHueIlxem:uaX\ldoF1cX[nIHHjeIl3cXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgRoNzNUGkbDD3bZRpKEmFNUCgc4YhOC5yMES1{txOM1vBOVI{ODh6NkS0
BA/F3M1;OW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2TaPFczKGh?MVvEUXNQMYXJcoR2[2W|IHHueIlxem:uaX\ldoF1cX[nIHHjeIl3cXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDCZ5IuSWKuIGSzNVVKKG23dHHueEB4cXSqIFnDOVAhd2ZiMT63NVTPxE1?MmXkNlMxQDh4NES=
BA/F3NYfu[lA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF\xU|c4OiCqMU\EUXNQNH21e2pKdmS3Y3XzJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiQlPSMWFDVCCINEi2V{BufXSjboSgZZN{\XO|ZXSgZZMh\3Kxd4ToJGlvcGmkaYTpc44hf2m2aDDJR|UxKG:oIECuNFAxQc7:TR?=NWn2cGtFOjN|MEG3NFM>
BA/F3NYDQfXJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUnzT|NtPzJiaB?=MoO3SG1UVw>?MWPJcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4PpcochSkOULVHCUEBGOjV3SzDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIFnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMECzNu69VQ>?NEDzSY8zOzNyMUewNy=>
BA/F3MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHzGSnI4OiCqNIPyeFJFVVORMn3FTY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEKFUj3BRmwhTzJ3MFWgcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDJcohq[mm2aX;uJJdqfGhiSVO1NEBw\iByLkCwOVHPxE1?MoqwNlM{ODF5MEO=
BA/F3Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NF:1VnE4OiCqM{\HcWROW09?MXXJcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4PpcochSkOULVHCUEBSOjV{SDDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIFnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMEC4{txONYLLRms5OjN|MEG3NFM>
BA/F3MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1PQOlczKGh?NF:3OY5FVVORM1O1Z2lv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKEV|NUnWJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFE{|ryPM13SdlI{OzBzN{Cz
BA/F3M4n0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFvGUHE4OiCqMYHEUXNQMX\JcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEKFUj3BRmwh[XO|ZYPz[YQh[XNiZ4Lve5RpKEmwaHnibZRqd25id3n0bEBKSzVyIH;mJFAvODBzOd88US=>NFXMR3AzOzNyMUewNy=>
BA/F3NEfNdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFLy[nI4OiCqMo\0SG1UVw>?MVzJcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4PpcochSkOULVHCUEB[OjV|SDDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIFnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMECyN:69VQ>?MmqxNlM{ODF5MEO=
BA/F3NUTkPXZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoP6O|IhcA>?NWXkfoFiTE2VTx?=M2jUZWlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKFR|MUXJJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMz62{txOMn[yNlM{ODF5MEO=
BA/F3M{\HXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{PsVlczKGh?M1vOOGROW09?MkjyTY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghUW6qaXLpeIlwdiC5aYToJGlEPTBib3[gNk42|ryPMVmyN|MxOTdyMx?=
T cellNHOzc5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M33mV|czKGh?MmDqSG1UVw>?NGLFNZBKdmirYnn0d{BidnSrIFPEN{0h[W6mIHHueIkhS0R{OD3pcoR2[2WmIGSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwN:69VQ>?MoL5NVcyPTR3MUK=
WiDrMlSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXOwdWttPzJiaB?=M1zwb2ROW09?MWPJR|UxRTBwMEWyJO69VQ>?NY\SVXNsOTV4MUW1NVI>
PC3NUfWcVhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF\RUpM4OiCqMW\EUXNQMV3JR|UxRTBwMEC5OEDPxE1?M1;xdlE2PjF3NUGy
MDA-MB-231NIP3S3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MU[3NkBpMlrGSG1UVw>?NEWzbmlKSzVyPUCuNFEzKM7:TR?=NIrveVgyPTZzNUWxNi=>
Hs578TM2TKUGN6fG:2b4jpZ{BCe3OjeR?=NV\6eml2PzJiaB?=MlfiSG1UVw>?NXHXcXFJT0l3ME2wMlA{KM7:TR?=M{TqRlI1ODF3M{K3
HMECMUfDfZRwfG:6aXOgRZN{[Xl?MkPuO|IhcA>?MVzEUXNQMULHTVUxRTFwODFOwG0>MnrENlQxOTV|Mke=
DU145MoGxR5l1d3SxeHnjJGF{e2G7NFj3dI44OiCqNGDjcJFFVVORM2n0S2dKPTB;MD6xOkDPxE1?NHXZPWwzPDBzNUOyOy=>
U251MWfDfZRwfG:6aXOgRZN{[Xl?MWq3NkBpNXLjc2xITE2VTx?=MXfHTVUxRTJwOEGg{txOMonhNlQxOTV|Mke=
NCI60MXLDfZRwfG:6aXOgRZN{[Xl?NEjzTY04OiCqM3fueWROW09?M1HUeGdKPTB;NT63JO69VQ>?MVeyOFAyPTN{Nx?=
MALME-3MMkP5R5l1d3SxeHnjJGF{e2G7MoPsO|IhcA>?NYrRN3dxTE2VTx?=NXzWTlZJT0l3ME22MlYyKM7:TR?=NF;HWlIzPDBzNUOyOy=>
KM12MorPR5l1d3SxeHnjJGF{e2G7NUGwOpR7PzJiaB?=NXm2ZodsTE2VTx?=MnLaS2k2OD15LkS0JO69VQ>?M1vSNFI1ODF3M{K3
SW620NGXsUmxEgXSxdH;4bYMhSXO|YYm=MWO3NkBpNYf6VVZWTE2VTx?=MmnUS2k2OD16LkSzJO69VQ>?M2TlT|I1ODF3M{K3
RXF 393NLNHfDc3ZEgXSxdH;4bYMhSXO|YYm=MY[0JIRigXN?MXfEUXNQNYLSOYVpUUN3ME2wMlAzOTdizszNNEi1XJQzOzJ3M{C3OC=>
LXFA 983LMXXDfZRwfG:6aXOgRZN{[Xl?NGGyPW41KGSjeYO=NXXufXQxTE2VTx?=Mm\lTWM2OD1yLkC1OlUh|ryPMnP4NlMzPTNyN{S=
PRXF DU145MlXHR5l1d3SxeHnjJGF{e2G7NITqVXc1KGSjeYO=NFy2OoNFVVORM1riO2lEPTB;MD6wOlI{KM7:TR?=MoXzNlMzPTNyN{S=
PAXF 1657LMXfDfZRwfG:6aXOgRZN{[Xl?MXG0JIRigXN?MX;EUXNQM1rnNGlEPTB;MD6xNlEh|ryPMmjtNlMzPTNyN{S=
CXF 1103LNFHUbmdEgXSxdH;4bYMhSXO|YYm=MYC0JIRigXN?MnfNSG1UVw>?MW\JR|UxRTRwM{[g{txONH\WUXUzOzJ3M{C3OC=>
GXF251LM1HYN2N6fG:2b4jpZ{BCe3OjeR?=MWm0JIRigXN?MW\EUXNQNH;BcpRKSzVyPUKuNlUh|ryPM3;sVVI{OjV|MEe0
NCI-H23MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M13tUFczKGh?MYPEUXNQMXvJR|UxRTJwMkeg{txOM{n0RVI{PTJzMEKw
HCT116MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NHjmbZc4OiCqM{nUc2ROW09?MXTJR|UxRTJwMzFOwG0>NV3SdGRKOjN3MkGwNlA>
MCF7NF3a[pBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWr6Z4tyPzJiaB?=NFyxc5lFVVORNVjUd2tCUUN3ME2yMlU4KM7:TR?=MUiyN|UzOTB{MB?=
NCI-H460MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmnZO|IhcA>?NWm3b5pVTE2VTx?=MWrJR|UxRThwOUmg{txONFLqUnYzOzV{MUCyNC=>
DLD1MoDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVi1UGN1PzJiaB?=NFrqZpRFVVORMYHJR|UxRTRwNjFOwG0>Ml3SNlM2Pjd7NkC=
NCI-H661NInTbVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NE\H[lA4OiCqNFvmRmJFVVORNUH3R3JGUUN3ME23Mlgh|ryPMof6NlM2Pjd7NkC=
A549MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnSyO|IhcA>?M33UOGROW09?M1G2b2lEPTB;OD6yJO69VQ>?NX3YNlg{OjN3Nke5OlA>
U937M3zjdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{HONlczKGh?M3LNV2ROW09?MljnTWM2OD1zMj6yJO69VQ>?MVSyN|U3Pzl4MB?=
HEK293NWPQN4J4TnWwY4Tpc44hSXO|YYm=MVuxNOKh|ryPNYfpOGpZTE2VTx?=NFLjVGNKdmS3Y3XzJIJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6g[pVtdC2uZX7neIghUGm|LYTh[4dm\CCPeYSxJItqdmG|ZTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IIfpeIghUUN3MDDv[kAxNjB4M988US=>Mnu4NlI4PzB4MUC=
HUVECNXzoTJl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmjlNE4yPcLizszNNWHiSJpVPzJiaB?=NILrPVhFVVORM1\nRmlv\HWlZYOgZY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliaX6gTHVXTUNiY3:tZ5VtfHW{ZXSge4l1cCC4YYPjeYxieiC|bX;veIghdXW|Y3zlJINmdGy|IHHzd4V{e2WmIHHzJGlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigZZQhOC5zNTD1US=>MWGyNlg2Ozl7Mx?=
HUVECNFe5NZFHfW6ldHnvckBCe3OjeR?=NWjoclVMOTYEoN88US=>NYH4fYxRPzJiaB?=MXfEUXNQNVjNPJVlUW6mdXPld{BidnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDpckBJXV[HQzDjc{1kfWy2dYLl[EB4cXSqII\hd4N2dGG{IIPtc491cCCvdYPjcIUh[2WubIOgZZN{\XO|ZXSgZZMhUW6qaXLpeIlwdiCxZjDu[ZR4d3KtIH\vdo1ifGmxbjDheEAyNjhidH:gNVUhfU1?MUOyNlg2Ozl7Mx?=
Plasmodium falciparumM2G4[WZ2dmO2aX;uJGF{e2G7Ml;KNVDDqM7:TR?=M4HWZVE2KG2rbh?=MWLEUXNQMWPJcohq[mm2czDQcIF{dW:maYXtJIZidGOrcHHyeY0heHKxbHnm[ZJifGmxbjDifUBqdmirYnn0bY5oKHSqZTDGeY5kfGmxbjDv[kBR\kOGUFuxJJBzd3SnaX6ge4l1cCCLQ{WwJI9nKDFwMUhOwG0>Mn\TNlQ2PTB|M{C=
PC3MoPqSpVv[3Srb36gRZN{[Xl?MmjkNE4yKM7:TR?=NITFWI82KGh?MVjEUXNQNXj6dVdRUW6qaXLpeJMhcHWvYX6gVGM{KGOnbHygZYRp\XOrb36gZZQhOTByIH7NMWSxPVQ3Ojl5NR?=
DU145NWH1e21nTnWwY4Tpc44hSXO|YYm=MmjLNE4yKM7:TR?=NEn6dJQ2KGh?NFnLNpBFVVORMoPsTY5pcWKrdIOgbJVu[W5iRGWxOFUh[2WubDDh[Ihme2mxbjDheEAyODBibl2=MXSxPVQ3Ojl5NR?=
PC3M{LWe2tqdmG|ZTDBd5NigQ>?MWKwMlEh|ryPMojlOUBpMoXnSG1UVw>?NXf2[FBJUW6qaXLpeJMh[1O{YzDpckBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIIDoc5NxcG:{eXzheIVlKFO{YzDZOFE3KGyndnXsJIF1KDFyMDDuUS=>NGHNRZEyQTR4Mkm3OS=>
DU145MmPPT4lv[XOnIFHzd4F6M2LTfFAvOSEQvF2=NYHkOJNuPSCqM3;qPGROW09?NISzVYtKdmirYnn0d{BkW3KlIHnuJIh2dWGwIFTVNVQ2KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDwbI9{eGixconsZZRm\CCVcnOgXVQyPiCuZY\lcEBifCBzMECgcm0>NHLIV2EyQTR4Mkm3OS=>
PC3MYnLbY5ie2ViQYPzZZk>M3vCZVAvOSEQvF2=M3\jNlUhcA>?MmniSG1UVw>?NFm1dm5KdmirYnn0d{BkW3KlIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZicHjvd5Bpd3K7bHH0[YQhTkGNIGm1O|YwYTV5NzDs[ZZmdCCjdDCxNFAhdk1?M4jufFE6PDZ{OUe1
DU145M2f2N2tqdmG|ZTDBd5NigQ>?M{HHbFAvOSEQvF2=NHnDO|c2KGh?NYKzUHE3TE2VTx?=MXzJcohq[mm2czDjV5JkKGmwIHj1cYFvKESXMUS1JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCyaH;zdIhwenmuYYTl[EBHSUtiWUW3Ok9[PTd5IHzleoVtKGG2IEGwNEBvVQ>?NF3w[5MyQTR4Mkm3OS=>
Huh7MnLtRY51cX[rcnHsJGF{e2G7NF3xZ2YzNjVizszNNELNeZA1KGSjeYO=M2\0RWROW09?M4H6cGlvcGmkaYTzJJZqemGuIIPwdoVi\CCrbjDE[Y5ofWVidnnyeZMucW6oZXP0[YQhcHWvYX6gTJVpPyClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gc4Yhfmm{YXyg[Y53\WyxcHWgdJJwfGWrbjD3bZRpcW5icHXybY52[2ynYYKgdoVocW:wIHH0JFIvPSC3TR?=NHH3XYUyPzN4ME[3Oi=>
C6/36MVTBcpRqfmm{YXygRZN{[Xl?NYq3UWhiOi53IN88US=>NYPnc5Y1PCCmYYnzM3vaSmROW09?MY\Jcohq[mm2czD2bZJidCC|cILlZYQhcW5iRHXu[5VmKH[rcoXzMYlv\mWldHXkJIF{cWGwIITp[4VzKG2xc4H1bZRwKEN4L{O2JINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCxZjD2bZJidCCnbo\lcI9x\SCycn;0[YlvKHerdHjpckBx\XKrboXjcIVieiC{ZXfpc44h[XRiMj61JJVOM3;CUFE4OzZyNke2
U937NUj2SJdVTnWwY4Tpc44hSXO|YYm=NHiwfHoyKM7:TR?=NGDXeIcyKGh?MXnEUXNQM4DaNHJm\HWlZYOgZoF{[WxiVF7GZYxxcGFicnXs[YF{\SCrbjDoeY1idiCXOUO3JINmdGy|M2faclE4Pjh2MEm5
U937MXrGeY5kfGmxbjDBd5NigQ>?NGj3WHoyKM7:TR?=M1vrclEhcA>?NFHKeZVFVVORM3;mbHJm\HWlZYOgUHBUNWmwZIXj[YQhXE6IYXzwbIEhemWuZXHz[UBqdiCqdX3hckBWQTN5IHPlcIx{NYD3c5I2OTd4OESwPVk>
murine mast cellMVHGeY5kfGmxbjDBd5NigQ>?M2HUN|Eh|ryPNIXX[pQzPCCqNHjtS3VFVVORNH:4bmVKdmirYnn0d{BidnSrZ3XuMYlv\HWlZXSgTWw3KHOnY4LleIlwdiCrbjDJ[2UheHKrbXXkJI1wfXOnIH3hd5Qh[2WubIOgZZQhOSC3TR?=NWSyN5VDOTd4OESwPVk>
BV-173MlvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NULZZlljUUN3ME2wMlAxODByMEGwPUDPxE1?NFjQfFZUSU6JRWK=
K-562M17VRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEDBWWtKSzVyPUCuNFAxODByMk[2JO69VQ>?NUe5VohOW0GQR1XS
BL-70NFyyeIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlTYTWM2OD1yLkCwNFAxODh{MjFOwG0>M13wbHNCVkeHUh?=
EM-2MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2PnXWlEPTB;MD6wNFAxODFyODFOwG0>MoDsV2FPT0WU
LAMA-84M4LTOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mmn4TWM2OD1yLkCwNFAxOzJzIN88US=>NWT2UnB[W0GQR1XS
MEG-01MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXHJ[nZzUUN3ME2wMlAxODByOUig{txOMl35V2FPT0WU
EoL-1-cellMVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXnUWnZ6UUN3ME2wMlAxODBzM{Gg{txOMni2V2FPT0WU
CTV-1NGm0c|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NITveFhKSzVyPUCuNFAxODRyNDFOwG0>NHPCZ|dUSU6JRWK=
TE-15MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXzJR|UxRTBwMEC1PFkh|ryPM{fwXHNCVkeHUh?=
NOS-1NITkS4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NE\GToNKSzVyPUCuNFA3OTNizszNMlrCV2FPT0WU
D-336MGMoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MYrJR|UxRTBwMEC2N{DPxE1?NX\V[mMyW0GQR1XS
LB1047-RCCMmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIXTfJZKSzVyPUCuNFA6QDlizszNNWLyZZc5W0GQR1XS
LB996-RCCNFWxXY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MX3JR|UxRTBwMEC5PVEh|ryPNX\KXG1yW0GQR1XS
SW982MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEH4TI1KSzVyPUCuNFEyOTVizszNNGXQcIRUSU6JRWK=
TK10MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MWrJR|UxRTBwMEGxO|Qh|ryPNFLMbXhUSU6JRWK=
A704NWLDXFlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1HZW2lEPTB;MD6wNVQ6OSEQvF2=M4Du[XNCVkeHUh?=
TE-8NX7nZmhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkW5TWM2OD1yLkCxOVc3KM7:TR?=M2nwRXNCVkeHUh?=
DOHH-2MlTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MYnJR|UxRTBwMEG3NVkh|ryPMUfTRW5ITVJ?
HOP-62NVuxU4VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVXRTYhWUUN3ME2wMlAyQDN2IN88US=>NFvNb|dUSU6JRWK=
TE-12MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUXVOotbUUN3ME2wMlAyQDZzIN88US=>NYXGXnFZW0GQR1XS
KGNM{fheGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVLJR|UxRTBwMEG5OFIh|ryPMXXTRW5ITVJ?
NCI-H1648MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2P0VWlEPTB;MD6wNlAyOSEQvF2=MWDTRW5ITVJ?
OS-RC-2Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2PFTWlEPTB;MD6wNlA{KM7:TR?=NWDSPVUyW0GQR1XS
GB-1MljRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mn;pTWM2OD1yLkCyNVU4KM7:TR?=MU\TRW5ITVJ?
RXF393MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXjKXIRmUUN3ME2wMlAzOzV5IN88US=>NX3vXZZYW0GQR1XS
LC-2-adNWPvVJVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnjyTWM2OD1yLkCyOVg3KM7:TR?=MYLTRW5ITVJ?
KS-1M3zBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2jxSGlEPTB;MD6wNlc{KM7:TR?=MXfTRW5ITVJ?
ETK-1MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUS4dHpoUUN3ME2wMlAzQDN{IN88US=>MmfsV2FPT0WU
SW954MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXXJR|UxRTBwMEK5Nlch|ryPNEjWcmxUSU6JRWK=
BeckerNGXTTINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MUPJR|UxRTBwMEOwNFMh|ryPM1XZOnNCVkeHUh?=
MZ1-PCNGjEd2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MWnJR|UxRTBwMEOxNVkh|ryPNYi3ZXFYW0GQR1XS
ES6NEHmR5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MoT6TWM2OD1yLkCzNVk{KM7:TR?=MXnTRW5ITVJ?
KURAMOCHIMW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mlm4TWM2OD1yLkCzOFg4KM7:TR?=M4rqW3NCVkeHUh?=
CGTH-W-1NXTtOohZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4OzU2lEPTB;MD6wN|U1QCEQvF2=MYHTRW5ITVJ?
VA-ES-BJM1vnVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1eydGlEPTB;MD6wN|kxOiEQvF2=MoLIV2FPT0WU
LXF-289MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYTsNGd5UUN3ME2wMlA{QTV4IN88US=>NXrRUIVuW0GQR1XS
MPP-89MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MnHpTWM2OD1yLkC0NFQ6KM7:TR?=NY\xVGsyW0GQR1XS
SW872MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NX3OOIN[UUN3ME2wMlA1OTZzIN88US=>M1TtbHNCVkeHUh?=
SNB75NX:wdm5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mn\GTWM2OD1yLkC0OFM2KM7:TR?=M3qxW3NCVkeHUh?=
PSN1MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2PkUWlEPTB;MD6wOFQ4PCEQvF2=NVvmZlA1W0GQR1XS
LB831-BLCMoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkLTTWM2OD1yLkC0OlA6KM7:TR?=M4jNOHNCVkeHUh?=
MFH-inoNW\4cotyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2fubWlEPTB;MD6wOFczPCEQvF2=NUTaV5RqW0GQR1XS
TGBC24TKBNUixbplwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVrJR|UxRTBwMES3OlEh|ryPMXzTRW5ITVJ?
A388NWDCW29GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXzJR|UxRTBwMEWwPVUh|ryPNEix[|RUSU6JRWK=
BB30-HNCMnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MXPJR|UxRTBwMEW0N|ch|ryPMl\tV2FPT0WU
GI-ME-NMUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{TPTWlEPTB;MD6wOlEyQCEQvF2=NFjHeZJUSU6JRWK=
TGBC1TKBNYjSdGl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHLlcpJKSzVyPUCuNFYyPjRizszNM2nYXnNCVkeHUh?=
TE-10M33FW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MULJR|UxRTBwME[zOVch|ryPNWLsfo5pW0GQR1XS
A498NULNWVRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4PmS2lEPTB;MD6wO|I5PCEQvF2=Mn\ZV2FPT0WU
TE-11NVXzc5ZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mkn1TWM2OD1yLkC3PFU5KM7:TR?=MU\TRW5ITVJ?
BB65-RCCNFjMTXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2rncmlEPTB;MD6wPFIzPyEQvF2=MXrTRW5ITVJ?
C2BBe1Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MV\JR|UxRTBwMEizNFgh|ryPNUSweGJTW0GQR1XS
NCI-H747NV3qVZhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MYHJR|UxRTBwMEizOlIh|ryPNF:5cHpUSU6JRWK=
IST-MES1NWjzPZE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWnJR|UxRTBwMEi1OVIh|ryPM1nYWXNCVkeHUh?=
KALS-1M4jR[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVHJR|UxRTBwMEm0PUDPxE1?NWS0T4h[W0GQR1XS
GCIYNX\Rc|FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUfWSVVtUUN3ME2wMlA6PjV4IN88US=>MXzTRW5ITVJ?
RL95-2MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkWxTWM2OD1yLkGwN|gh|ryPMmCyV2FPT0WU
TE-1MlnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{DlZWlEPTB;MD6xNFU1KM7:TR?=MXzTRW5ITVJ?
NCI-H1355M1nZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlvwTWM2OD1yLkGxNFI5KM7:TR?=MoHYV2FPT0WU
SW962NXrVV2dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mn3PTWM2OD1yLkGxNlkzKM7:TR?=MlnMV2FPT0WU
KLEMkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYLDdHJ2UUN3ME2wMlEyOzF5IN88US=>M13HbHNCVkeHUh?=
MC116NYrYeGpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NI\4cWVKSzVyPUCuNVE1OSEQvF2=NIfUV4dUSU6JRWK=
NMC-G1NYrRZplMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1X6bmlEPTB;MD6xNVYxPiEQvF2=MUPTRW5ITVJ?
KU812NVK1PHlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MU\JR|UxRTBwMUG4PFMh|ryPM1v0V3NCVkeHUh?=
COLO-829Mlj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYXHWYw3UUN3ME2wMlEzOjF|IN88US=>NGn2NZJUSU6JRWK=
NTERA-S-cl-D1NFzVdlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NX6wTmVtUUN3ME2wMlEzOjh|IN88US=>M3fGPHNCVkeHUh?=
IST-MEL1NUPCb3k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVLPNGJ5UUN3ME2wMlE{PDVizszNMojnV2FPT0WU
MLMAMXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEXzUm1KSzVyPUCuNVQxOzJizszNMYDTRW5ITVJ?
LS-123M3rWTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{S1b2lEPTB;MD6xOFA3PCEQvF2=NGTUb2pUSU6JRWK=
LB2518-MELM1rwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlzsTWM2OD1yLkG0NVYzKM7:TR?=MXXTRW5ITVJ?
NB69M13xdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MY\JR|UxRTBwMUS0N|Yh|ryPNHO0TpFUSU6JRWK=
8-MG-BAM3X5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWLJR|UxRTBwMUW0OVgh|ryPM{\VNnNCVkeHUh?=
K5NGDtS5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MV7JR|UxRTBwMU[0PFkh|ryPNHP3XXJUSU6JRWK=
KINGS-1NWX1XlRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHX3O4JKSzVyPUCuNVY3PjZizszNNY\SdXFqW0GQR1XS
SF268NV\6dY9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NH;pSIFKSzVyPUCuNVc1ODRizszNMXHTRW5ITVJ?
PF-382M{jWVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3rPdmlEPTB;MD6xO|Y4QCEQvF2=NX7WNIxJW0GQR1XS
SH-4NY\xO3Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3jSTGlEPTB;MD6xPFQyOyEQvF2=MknXV2FPT0WU
NALM-6M1z3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGm0PJFKSzVyPUCuNVkzQTVizszNM3zxdnNCVkeHUh?=
CP66-MELMn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkT2TWM2OD1yLkG5OVMyKM7:TR?=Moq5V2FPT0WU
697M4nQcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVTJR|UxRTBwMUm5PFch|ryPMVXTRW5ITVJ?
CP67-MELMo\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIDhe5RKSzVyPUCuNlA1QDhizszNMlz4V2FPT0WU
DSH1MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUfRVFk2UUN3ME2wMlI1ODBzIN88US=>NWn2T|g{W0GQR1XS
HCE-4Mm\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFrld3ZKSzVyPUCuNlY1OzlizszNNH7SfYhUSU6JRWK=
MZ2-MELMnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MX;JR|UxRTBwMki1N|ch|ryPM4r4XnNCVkeHUh?=
BL-41NFLnWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmD3TWM2OD1yLkK5NVI{KM7:TR?=NHzlfJpUSU6JRWK=
HUTU-80MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3PuOWlEPTB;MD6zNVQzKM7:TR?=NFvwO2VUSU6JRWK=
LOXIMVINHr2NpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MULJR|UxRTBwM{G1NFMh|ryPMYjTRW5ITVJ?
no-10NUTaWJN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmP6TWM2OD1yLkOxPVMyKM7:TR?=M3zqVHNCVkeHUh?=
KARPAS-422MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWHtNWtpUUN3ME2wMlM{QTl5IN88US=>NVL1RYtxW0GQR1XS
SW684MmDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVnPd3NHUUN3ME2wMlM1QThizszNMl2wV2FPT0WU
SF126M3TtXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVLJR|UxRTBwM{W0NUDPxE1?MVfTRW5ITVJ?
D-263MGM4P1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1vjVGlEPTB;MD6zOlIzPCEQvF2=NImwWWZUSU6JRWK=
OVCAR-4NHTjRZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYf0PVJlUUN3ME2wMlM4PDN|IN88US=>NYjve3ZyW0GQR1XS
BB49-HNCNHX1TXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGLEXVRKSzVyPUCuN|g2QTlizszNNHzKcmxUSU6JRWK=
ONS-76M3XrfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYXJR|UxRTBwNEK5OVEh|ryPMofqV2FPT0WU
MZ7-melNGTXVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWTUVXB2UUN3ME2wMlQ4QTFzIN88US=>NIXjWodUSU6JRWK=
RCC10RGBNUnCdJdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFfpO45KSzVyPUCuOFkyOSEQvF2=MlXKV2FPT0WU
BOKUM{fnfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnTkTWM2OD1yLkS5NVM{KM7:TR?=NGf6bpRUSU6JRWK=
no-11Mn7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2DPeGlEPTB;MD61NFIzQCEQvF2=NFr2TGZUSU6JRWK=
IST-SL2NIrmdHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmniTWM2OD1yLkWwN|AzKM7:TR?=NGTvZWdUSU6JRWK=
RKOMY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVzaS2hsUUN3ME2wMlUzQTZ4IN88US=>NFnvUGRUSU6JRWK=
HT-144M2GwVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NV;wPHFpUUN3ME2wMlU{PjB7IN88US=>MknmV2FPT0WU
NCI-H446MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXzJR|UxRTBwNkK3OkDPxE1?MkG3V2FPT0WU
QIMR-WILNVnJ[Jl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4HpcGlEPTB;MD63NFYzQSEQvF2=NXPEVXkyW0GQR1XS
MHH-PREB-1NGLBTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYLlNGFZUUN3ME2wMlc1PDZ7IN88US=>M2PxXHNCVkeHUh?=
EW-16M2\KXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFPVdY9KSzVyPUCuO|YyPzhizszNNF3zWnNUSU6JRWK=
EW-24NG\DbFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGS0NWtKSzVyPUCuO|gyPjVizszNNUXXfmpxW0GQR1XS
LB373-MEL-DNXLwUJY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3HF[mlEPTB;MD64NlUxQCEQvF2=Mn:0V2FPT0WU
TE-9NFrWWXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHv0Z5ZKSzVyPUCuPFc2OzJizszNMnnCV2FPT0WU
A3-KAWMYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{Pt[WlEPTB;MD65PFQ2OiEQvF2=MnfxV2FPT0WU
A101DM1rXPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MX3JR|UxRTFwMEOwOFMh|ryPNUfIbY46W0GQR1XS
OCUB-MNGrzOFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlPSTWM2OD1zLkC0OFEzKM7:TR?=M{K2bXNCVkeHUh?=
ES4NXPwfnNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVPJR|UxRTFwMEWxOFUh|ryPMoXlV2FPT0WU
TE-6NYmw[W45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoXHTWM2OD1zLkKxNlI3KM7:TR?=NUfiNolYW0GQR1XS
D-502MGNFzUNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MYTJR|UxRTFwMkOzO|Yh|ryPMlG4V2FPT0WU
KNS-42NYXDU4VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3v2XWlEPTB;MT6yOFQyOiEQvF2=MVPTRW5ITVJ?
SNU-C2BMXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVPBPXZmUUN3ME2xMlMxPTh7IN88US=>NH\KNFlUSU6JRWK=
NCI-H1838M4ixWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{XreGlEPTB;MT6zNFc{OyEQvF2=NFWzeJhUSU6JRWK=
NKM-1NFfDZ29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGTsZ5dKSzVyPUGuN|A5PTlizszNMXrTRW5ITVJ?
GI-1NWLEc3ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3HofmlEPTB;MT6zOlIzKM7:TR?=NEfBNGZUSU6JRWK=
NB5NWTnOIlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkTITWM2OD1zLkO5PFI4KM7:TR?=NEnDd41USU6JRWK=
CAS-1Ml\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUXJR|UxRTFwNEC5PVIh|ryPMV3TRW5ITVJ?
HCE-TNEfXTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3vvd2lEPTB;MT61OlcyPCEQvF2=NF3vfXZUSU6JRWK=
SBC-1NVXsXWhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHG4SmRKSzVyPUGuOVc6QDRizszNM3P3SXNCVkeHUh?=
JiyoyeP-2003M2TXVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHvXSmdKSzVyPUGuO|M1PjZizszNNILHV29USU6JRWK=
TE-5MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1rJRmlEPTB;MT63PVE{QSEQvF2=NFXBRYhUSU6JRWK=
CANM3m0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MV\JR|UxRTFwOEKyOVIh|ryPMXnTRW5ITVJ?
SK-UT-1M2jzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4LRUmlEPTB;Mj6xOlY6OyEQvF2=NFLJU|RUSU6JRWK=
JVM-2MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{mxXmlEPTB;Mj6zOlI5PCEQvF2=MmnQV2FPT0WU
LB771-HNCMVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUnJR|UxRTJwNUe1OVEh|ryPNUnBcIwyW0GQR1XS
NCCITMXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIq3XodKSzVyPUKuPFY3OTZizszNMWDTRW5ITVJ?
NCI-H2126MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWq1RnhVUUN3ME2yMlg4PTV{IN88US=>MWXTRW5ITVJ?
Calu-6NUnwRpp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHO1XJRKSzVyPUOuNFU4PDFizszNM{nTdnNCVkeHUh?=
SK-LMS-1MlHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIe1NmdKSzVyPUOuNVE5QDZizszNMnPuV2FPT0WU
ARH-77NEDX[|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M360bmlEPTB;Mz60OlkyPSEQvF2=MYTTRW5ITVJ?
NB17NF;5bmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3ryVmlEPTB;Mz62N|g1PyEQvF2=NGTkPZdUSU6JRWK=
A253M13tXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3vOWWlEPTB;Mz63N|I1PiEQvF2=NUf0epo5W0GQR1XS
OPM-2NIPpcIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NV;hOGg6UUN3ME20MlI4Pjh3IN88US=>NHXhNVFUSU6JRWK=
MV-4-11NEDjWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NH7BVZhKSzVyPUSuN|Y1PTRizszNNXjBcWRoW0GQR1XS
SRNX3CcnA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NGTMboFKSzVyPUSuOFk6PTRizszNM3jCVXNCVkeHUh?=
KG-1M{f6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlKxTWM2OD12Lk[wPFQ2KM7:TR?=NVTHUJQ3W0GQR1XS
OCI-AML2MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIfGNFZKSzVyPUWuPFYyPTRizszNMkXWV2FPT0WU
D-247MGM1XOSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mlm1TWM2OD14LkGyOVE6KM7:TR?=MmP5V2FPT0WU
DJM-1M1L4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2rUNWlEPTB;Nj60PFU2QCEQvF2=NXPK[HVCW0GQR1XS
RPMI-6666M2XHWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYLJR|UxRTdwMkewOlch|ryPMV\TRW5ITVJ?
KARPAS-45NUnIPHpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MlzETWM2OD15LkWxOlcyKM7:TR?=M3Wzd3NCVkeHUh?=
LP-1MlLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIG4NYlKSzVyPUeuOVQ4QDJizszNNEXqU4tUSU6JRWK=
RS4-11NFfIOVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlnMTWM2OD15Lk[1O|g4KM7:TR?=M{Txc3NCVkeHUh?=
DU-4475NGHHSm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{jSbGlEPTB;OD6yNVY2OiEQvF2=MlThV2FPT0WU
MONO-MAC-6MnnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1\lT2lEPTB;OD6yO|A3PiEQvF2=MXHTRW5ITVJ?
NCI-SNU-16M3\3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEXzPG1KSzVyPUiuOVYyOjhizszNMYnTRW5ITVJ?
SJSA-1M37zUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIPCXHhKSzVyPUiuO|I5ODVizszNMoq0V2FPT0WU
MMAC-SFMWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlLXTWM2OD16Lke5N|A4KM7:TR?=NGrJRYVUSU6JRWK=
SK-NEP-1NEDrTYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MX;JR|UxRThwOEmxOVUh|ryPM4r1R3NCVkeHUh?=
J-RT3-T3-5M4jucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIf1bJdKSzVyPUiuPVY2OjlizszNMV;TRW5ITVJ?
SKM-1M1T5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHjscoJKSzVyPUmuNFE4OzRizszNNWPaTodOW0GQR1XS
LB2241-RCCNYrSWYNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUHJR|UxRTlwMEKwNVIh|ryPMn3WV2FPT0WU
SIG-M5NHy2NlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnjuTWM2OD17LkCyOFk{KM7:TR?=NXXWTpBIW0GQR1XS
EVSA-TNG\R[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVzKTVhzUUN3ME25MlI4Pzl|IN88US=>MVvTRW5ITVJ?
GT3TKBM1\nZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYTHVGhMUUN3ME25MlM2PTR4IN88US=>M{OwbnNCVkeHUh?=
NB6NVXwRXNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFnOWVhKSzVyPUmuPVIzPTlizszNMXHTRW5ITVJ?
EHEBM2XYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYjzOnZHUUN3ME2xNE4xPjV4IN88US=>MY\TRW5ITVJ?
HELNUDqcnhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVPJR|UxRTFyLkS3O|Yh|ryPNUnPSYU5W0GQR1XS
ALL-PONF;nZ3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXe5fmE5UUN3ME2xNE44QTN6IN88US=>MmrGV2FPT0WU
TGWMVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkmxTWM2OD1zMT6yPFI5KM7:TR?=NFy5R|lUSU6JRWK=
BC-3NX2xdm95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVzJR|UxRTF{LkGxN|gh|ryPNXXGeWFrW0GQR1XS
IA-LMM3zvdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M37h[WlEPTB;MUKuOFQ1PSEQvF2=MnfFV2FPT0WU
UACC-257NYrjRpJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkjDTWM2OD1zMj65NVk5KM7:TR?=NIjn[IVUSU6JRWK=
KP-N-YSMXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1;EVmlEPTB;MUKuPVI5OyEQvF2=MWHTRW5ITVJ?
RajiM3G3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlrTTWM2OD1zMz63OFk4KM7:TR?=NWnFO491W0GQR1XS
SF539NYjOSoFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWDJR|UxRTF|Lki1OVch|ryPNYnJSVdNW0GQR1XS
DMS-153NWjVdHVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MlT2TWM2OD1zND6wNFI5KM7:TR?=NVfYN|RDW0GQR1XS
L-540M1rmT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlXzTWM2OD1zNT6wOlczKM7:TR?=MWLTRW5ITVJ?
MN-60NVzOVXFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Ml3BTWM2OD1zNT6xPVc6KM7:TR?=NGm2Rm5USU6JRWK=
RPMI-8866MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2DkOWlEPTB;MUeuOFQ2PCEQvF2=NWWxToxvW0GQR1XS
NCI-H510ANFTiTVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVGyNGI5UUN3ME2xPU4{QTd|IN88US=>NG\ZRYRUSU6JRWK=
NB13MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIXCTlNKSzVyPUG5MlQ5PzdizszNMV7TRW5ITVJ?
HAL-01MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mlu3TWM2OD1zOT63OVQ{KM7:TR?=MUjTRW5ITVJ?
NCI-H720MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mnf3TWM2OD1{MD6yO|M{KM7:TR?=M2\3dXNCVkeHUh?=
REHNIf5d|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFnC[FBKSzVyPUKwMlY{PTdizszNMkTmV2FPT0WU
KNS-81-FDMXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4rvUGlEPTB;MkOuNVQ3KM7:TR?=M{nNOHNCVkeHUh?=
HC-1M{XON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{XieGlEPTB;MkSuOVU2OSEQvF2=NHT0W2RUSU6JRWK=
NCI-H2141M3X4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFLFTZJKSzVyPUK0Mlc4PTRizszNMVHTRW5ITVJ?
MOLT-4MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnvFTWM2OD1{Nj62O|U{KM7:TR?=NGf0VJJUSU6JRWK=
OMC-1NIWzdYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHvzRZRKSzVyPUK3MlE1OjJizszNNXXIRVJXW0GQR1XS
LC-1FMn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{PpSGlEPTB;MkeuN|I1PSEQvF2=MmXBV2FPT0WU
NCI-H1304MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MknPTWM2OD1{OD6xOlI5KM7:TR?=NF\YUJdUSU6JRWK=
BC-1M4q0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmDxTWM2OD1{OD62OVEh|ryPNXLmXHQ5W0GQR1XS
NCI-H64M3nlTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGDrOYJKSzVyPUK5MlYzPTNizszNMl;HV2FPT0WU
MOLT-16MnfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MX7JR|UxRTJ7Lk[yPVIh|ryPNU[4RWxDW0GQR1XS
U-87-MGNF\aR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4izbGlEPTB;M{CuO|Y3KM7:TR?=M{fDe3NCVkeHUh?=
GAKM37HTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEjKeXZKSzVyPUOxMlI3QDZizszNM1XZR3NCVkeHUh?=
ES8NGP1ZZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1rqdGlEPTB;M{KuNVI2OiEQvF2=MoHMV2FPT0WU
HCC1599MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M37QPGlEPTB;M{KuN|MzPSEQvF2=NXzFTJdbW0GQR1XS
EB-3NUfDfYtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXzJR|UxRTN2LkOxNVch|ryPNIfa[G5USU6JRWK=
HCC1187M1TCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1zBZ2lEPTB;M{WuPFA2OiEQvF2=M2njUXNCVkeHUh?=
SK-PN-DWMlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MWjJR|UxRTN4LkG5OFMh|ryPNFLZN21USU6JRWK=
JVM-3MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NED3Zm5KSzVyPUO3MlI{OzhizszNM{XUVHNCVkeHUh?=
HCC2157NVzuT2pjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUPJR|UxRTN5Lkm5OFYh|ryPMW\TRW5ITVJ?
A4-FukNXXuTI17T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFHjdmRKSzVyPUO4MlExODlizszNMWLTRW5ITVJ?
COR-L279NVzGNmZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NEnT[5pKSzVyPUSwMlI5PTFizszNM1;Vd3NCVkeHUh?=
DELMnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkTpTWM2OD12MT65NFg3KM7:TR?=MXXTRW5ITVJ?
NCI-H1395MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUPVWHZqUUN3ME20Nk4xOTZ|IN88US=>M1nyU3NCVkeHUh?=
MHH-NB-11NVrtelg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3zFV2lEPTB;NEOuNFgyQCEQvF2=MkfMV2FPT0WU
NCI-H2107NWDMWFFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{LmT2lEPTB;NEOuOFg1PiEQvF2=NYjNbm8{W0GQR1XS
NEC8MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NYKyWolVUUN3ME20OE4{OzZizszNNV32NWVLW0GQR1XS
COLO-684MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1\zU2lEPTB;NE[uNlI2QCEQvF2=NUfWXXVRW0GQR1XS
LS-411NMkntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlTLTWM2OD12OD60O|Q5KM7:TR?=MlnkV2FPT0WU

... 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 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02744768 Not yet recruiting Acute Lymphoblastic Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto June 2016 Phase 2
NCT02709083 Not yet recruiting Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive Emory University May 2016 Phase 2
NCT02720185 Not yet recruiting Breast Neoplasms|Triple Negative Breast Neoplasms University of Wisconsin, Madison|National Cancer Institut  ...more University of Wisconsin, Madison|National Cancer Institute (NCI) April 2016 Phase 2
NCT02750514 Not yet recruiting Advanced Cancer Bristol-Myers Squibb April 2016 Phase 2
NCT02596828 Recruiting Pineoblastoma University of Regensburg April 2016 Phase 2

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