Dasatinib (BMS-354825)

Catalog No.S1021 Synonyms: BMS-354825

For research use only.

Dasatinib (BMS-354825) 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. Dasatinib induces autophagy and apoptosis with anti-tumor activity.

Dasatinib (BMS-354825) Chemical Structure

CAS No. 302962-49-8

Selleck's Dasatinib (BMS-354825) has been cited by 470 publications

Purity & Quality Control

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Biological Activity

Description Dasatinib (BMS-354825) 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. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
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)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
M07ep210 NGTkS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL6eFIxPzJiaB?= M2XuWWROW09? M3z6d2lEPTB;MD6wNFAxPyEQvF2= NIXScIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{m1OlA5OCd-MUe5OVYxQDB:L3G+
K562 NES4cINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnqwO|IhcA>? M120ZmROW09? NHrCPZhKSzVyPUCuNFAyKM7:TR?= M1PCNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUW2NFgxLz5zN{m1OlA5ODxxYU6=
M07e NGP1d3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDRO|IhcA>? MWfEUXNQ M33zd2lEPTB;MD6wNFEzKM7:TR?= NF3pfoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{m1OlA5OCd-MUe5OVYxQDB:L3G+
ALL3 NIDsOHdEgXSxdH;4bYMhSXO|YYm= NXf6SlNSOC5zzszN MUG3NkBp NX;tSnVQTE2VTx?= NH2xV2hKSzVyPUCuNFAxPCEQvF2= M4e4fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEi5OVQxLz5zOUi4PVU1ODxxYU6=
CML NFTlXFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\4[|UzOCCvaX6= NFvKc5VFVVOR NF3lenNKSzVyPUCuNFAyKM7:TR?= M4XHRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkG5NFE3Lz5zOUKxPVAyPjxxYU6=
BA/F3 NI\vb4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fSbFczKGh? NIjYZ|hFVVOR MVnJR|UxRTZwNUi5JO69VQ>? NGHzc449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C4PFY1PCd-MkOwPFg3PDR:L3G+
BA/F3 NHq4T21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYD2Z2RGPzJiaB?= MXnEUXNQ NVrO[HNnUW6mdXPld{BidnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4PpcochSmO{LVHicEBOOzVzVDDteZRidnRid3n0bEBKSzVyIH;mJFAvODByOEROwG0> M3GyVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEi4OlQ1Lz5{M{C4PFY1PDxxYU6=
BA/F3 NHfKXY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUC3NkBp M1H0bmROW09? NX75c4FTUW6mdXPld{BidnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEKlcj3BZowhf2m2aDDJR|UxKG:oIECuNFA1Pc7:TR?= MljDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyOEi2OFQoRjJ|MEi4OlQ1RC:jPh?=
BA/F3 M2H0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXBO|IhcA>? MkXLSG1UVw>? MU\JcoR2[2W|IHHueIlxem:uaX\ldoF1cX[nIHHjeIl3cXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDCZ5IuSWKuIGSzNVVKKG23dHHueEB4cXSqIFnDOVAhd2ZiMT63NVTPxE1? NUT6Z3c1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwPFg3PDRpPkKzNFg5PjR2PD;hQi=>
BA/F3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f1RVczKGh? Mlu1SG1UVw>? NWD5R5kzUW6mdXPld{BkgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFLDVk1CSkxiRkS4OnMhdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBKdmirYnn0bY9vKHerdHigTWM2OCCxZjCwMlAxODoQvF2= NYrzbpVjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4ODNpPkKzN|AyPzB|PD;hQi=>
BA/F3 NE\3b5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPWO|IhcA>? MYTEUXNQ MoPGTY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEKFUj3BRmwhTTJ3NVugcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDJcohq[mm2aX;uJJdqfGhiSVO1NEBw\iByLkCwN|LPxE1? NInscIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVcxOyd-MkOzNFE4ODN:L3G+
BA/F3 MmHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK3NkBp MlTLSG1UVw>? NWXjbYdGUW6mdXPld{BkgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFLDVk1CSkxiR{K1NGUhdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBKdmirYnn0bY9vKHerdHigTWM2OCCxZjCwMlAxPTIQvF2= M36zV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CxO|A{Lz5{M{OwNVcxOzxxYU6=
BA/F3 NH73c4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\hO|IhcA>? NUTCbJF2TE2VTx?= NVvkUpZOUW6mdXPld{BkgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFLDVk1CSkxiUUK1NmghdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBKdmirYnn0bY9vKHerdHigTWM2OCCxZjCwMlAxQM7:TR?= NWXDZlNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4ODNpPkKzN|AyPzB|PD;hQi=>
BA/F3 MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjFWYI4OiCq NFvqXI9FVVOR NVTIW|RVUW6mdXPld{BkgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFLDVk1CSkxiRUO1PXYhdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBKdmirYnn0bY9vKHerdHigTWM2OCCxZjCwMlAxOTQQvF2= NVHXd4d4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4ODNpPkKzN|AyPzB|PD;hQi=>
BA/F3 NHLtN5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPPXVY4OiCq NFTEPYNFVVOR NXvzNGJuUW6mdXPld{BkgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDCR3IuSUKOIHHzd4V{e2WmIHHzJIdzd3e2aDDJcohq[mm2aX;uJJdqfGhiSVO1NEBw\iByLkCwNVnPxE1? M3O1WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CxO|A{Lz5{M{OwNVcxOzxxYU6=
BA/F3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfQemo4OiCq MnLqSG1UVw>? M17Eemlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKFl{NUPIJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFI{|ryP MlzxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEG3NFMoRjJ|M{CxO|A{RC:jPh?=
BA/F3 NIjRRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;ofFY4OiCq NEezW3lFVVOR M{myWWlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKFR|MUXJJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMz62{txO M37sUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CxO|A{Lz5{M{OwNVcxOzxxYU6=
BA/F3 NFHqd4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnvbZFkPzJiaB?= NGTwWIJFVVOR MnzWTY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghUW6qaXLpeIlwdiC5aYToJGlEPTBib3[gNk42|ryP MkC4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEG3NFMoRjJ|M{CxO|A{RC:jPh?=
T cell MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXRZ|I4OiCq NX;TZ4FvTE2VTx?= MXPJcohq[mm2czDhcpRqKEOGMz2gZY5lKGGwdHmgR2QzQC2rbnT1Z4VlKFRiY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjByM988US=> NWXjUYR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexOVQ2OTJpPkG3NVU1PTF{PD;hQi=>
WiDr MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWq3NkBp NYXsbIs2TE2VTx?= MlvQTWM2OD1yLkC1NkDPxE1? NIfkVmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNU[xOVUyOid-MUW2NVU2OTJ:L3G+
PC3 NYjTdHpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTLeZg4OiCq M3PEZmROW09? M4PpV2lEPTB;MD6wNFk1KM7:TR?= Mn7DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV4MUW1NVIoRjF3NkG1OVEzRC:jPh?=
MDA-MB-231 NGjpfopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3n4V|czKGh? MXvEUXNQ MonOTWM2OD1yLkCxNkDPxE1? NVX1fG5lRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW2NVU2OTJpPkG1OlE2PTF{PD;hQi=>
Hs578T MVLDfZRwfG:6aXOgRZN{[Xl? NEXDeII4OiCq M1vQZWROW09? NGfVVZRIUTVyPUCuNFMh|ryP NIrnW2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECxOVMzPyd-MkSwNVU{Ojd:L3G+
HMEC NF:yR5lEgXSxdH;4bYMhSXO|YYm= MWS3NkBp MX3EUXNQ NHPxXZJIUTVyPUGuPEDPxE1? NFXvXok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECxOVMzPyd-MkSwNVU{Ojd:L3G+
DU145 M4\0U2N6fG:2b4jpZ{BCe3OjeR?= MUe3NkBp NEPxOIpFVVOR MYHHTVUxRTBwMU[g{txO NYLLd3l6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVU{OjdpPkK0NFE2OzJ5PD;hQi=>
U251 NV71OIVVS3m2b4TvfIlkKEG|c3H5 MUi3NkBp M4HxN2ROW09? MkD2S2k2OD1{LkixJO69VQ>? NXe5XplWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVU{OjdpPkK0NFE2OzJ5PD;hQi=>
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MALME-3M MlTuR5l1d3SxeHnjJGF{e2G7 MUe3NkBp M3nE[mROW09? NEnmfoxIUTVyPU[uOlEh|ryP NXXrbYtDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVU{OjdpPkK0NFE2OzJ5PD;hQi=>
KM12 MVrDfZRwfG:6aXOgRZN{[Xl? MoPzO|IhcA>? MmnUSG1UVw>? NX25N21CT0l3ME23MlQ1KM7:TR?= M1nIflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEG1N|I4Lz5{NECxOVMzPzxxYU6=
SW620 NEDzW5hEgXSxdH;4bYMhSXO|YYm= NGrQ[VM4OiCq M2PKPWROW09? NWC2RYF2T0l3ME24MlQ{KM7:TR?= NEPDfY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECxOVMzPyd-MkSwNVU{Ojd:L3G+
RXF 393NL M1TDR2N6fG:2b4jpZ{BCe3OjeR?= Mmf2OEBl[Xm| M4TDPGROW09? NVK1XmJ[UUN3ME2wMlAzOTdizszN MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3M{C3OEc,OjN{NUOwO|Q9N2F-
LXFA 983L NInZVW9EgXSxdH;4bYMhSXO|YYm= MUm0JIRigXN? NITRTmJFVVOR NFHnNmtKSzVyPUCuNFU3PSEQvF2= NUP5XVgxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVMxPzRpPkKzNlU{ODd2PD;hQi=>
PRXF DU145 M3;XPGN6fG:2b4jpZ{BCe3OjeR?= M3nuelQh\GG7cx?= NUfYVIVZTE2VTx?= NIP5OlZKSzVyPUCuNFYzOyEQvF2= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3M{C3OEc,OjN{NUOwO|Q9N2F-
PAXF 1657L MXXDfZRwfG:6aXOgRZN{[Xl? MlH2OEBl[Xm| MXPEUXNQ M{\ESmlEPTB;MD6xNlEh|ryP M4fk[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkWzNFc1Lz5{M{K1N|A4PDxxYU6=
CXF 1103L NVThO|JtS3m2b4TvfIlkKEG|c3H5 NVPTdFJCPCCmYYnz NUW1UXE2TE2VTx?= M1HpZWlEPTB;ND6zOkDPxE1? NWjSfZNFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVMxPzRpPkKzNlU{ODd2PD;hQi=>
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NCI-H23 MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:5O|IhcA>? NFvYcpNFVVOR MnrnTWM2OD1{LkK3JO69VQ>? M1rkVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUKxNFIxLz5{M{WyNVAzODxxYU6=
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Assay
Methods Test Index PMID
Western blot phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) ; p27 / p21 ; p-FAK / p-STAT3 ; cleaved caspase 3 23049975 20145167 23721490
Growth inhibition assay IC50 23721490
Immunofluorescence SRC / Met ; F-actin / Actinin-4 / Paxillin ; α-tubulin 26517812 31053734
ELISA TNF-α ; E-selectin ; VCAM-1 17684099 31110200
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]

Protocol (from 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 Research:

[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 Research:

[3]

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

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 488.01
Formula

C22H26ClN7O2S

CAS No. 302962-49-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05198843 Recruiting Drug: Dasatinib|Dietary Supplement: Icosapent Ethyl Anatomic Stage IV Breast Cancer AJCC v8|Metastatic Triple-Negative Breast Inflammatory Carcinoma National Cancer Institute (NCI) March 25 2022 Phase 1|Phase 2
NCT04925648 Recruiting Drug: Dasatinib|Drug: Darolutamide Metastatic Prostate Cancer St Vincent''s Hospital Sydney October 18 2021 Phase 2
NCT04933526 Recruiting Drug: Flumatinib|Drug: Dasatinib Chronic Myeloid Leukemia in Chronic Phase Shenzhen Second People''s Hospital July 1 2021 Phase 4
NCT05433896 Completed Drug: Dasatinib ASD|Drug: Omeprazole 40 MG Pharmacokinetics|Drug Interactions Xspray Pharma AB|Axis Clinicals Limited November 1 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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Frequently Asked Questions

Question 1:
what’s the difference between S1021 and S7782? Which one is better for in vivo studies?

Answer:
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than hydrate one (S7782).

Question 2:
Can I give dasatinib to mice by oral gavage? If so, how to dissolve the drug?

Answer:
Our S1021 Dasatinib in 1% DMSO+30% PEG 300+1% Tween 80 at 30 mg/ml is a suspension which you can administrate to mice via oral gavage. If you want a clear solution, it can be dissolved in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5 mg/ml clearly.

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