Imatinib (STI571)

Catalog No.S2475 Synonyms: CGP057148B, ST-1571

Imatinib (STI571) Chemical Structure

Molecular Weight(MW): 493.6

Imatinib (STI571) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.

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Cited by 35 Publications

6 Customer Reviews

  • Ba/F3-p210T315I cells were treated with indicated concentrations of imatinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

    FASEB J 2011 25, 3661-3673. Imatinib (STI571) purchased from Selleck.

    Targeting KITLG through c-KIT inhibition using Imatinib; one representative experiment is shown (n = 4).

    Oncotarget, 2016, 7(34):54583-54595. Imatinib (STI571) purchased from Selleck.

  •  

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with imatinib. K562 cells (a and c) and MEG-01 cells (b and d) were incubated at 37 ◦C for 15 min with imatinib transport buffer, and then incubated with 0.5 Ci of [3H] thymidine or [3H] cytarabine for an additional 5 min in presence of imatinib. Cells were then washed 3 times, lysed and radioactivity associated to cell pellets was quantified. DMSO, dimethylsulfoxide; DPD, dipyridamole.

    Leukemia Res 2012 36, 1311-1314. Imatinib (STI571) purchased from Selleck.

    ZFX regulates imatinib sensitivity and PI3K/Akt signaling pathway in CML cells. Viability of cells transfected with si-ZFX at the indicated doses of imatinib for 24 h (a). Colonies of leukemia cells and imatinib-resistant cells transfected with si-ZFX following treatment with imatinib for 10 days (b). Western blot analysis of Akt, p-Akt, CyclinD1, CyclinE1, Bcl-2, and Caspase-3 in K562 and K562/G01 cells transfected with si-ZFX for 2 days (c). The relative densities of proteins were quantified and normalized to b-Actin (d). Values represented the mean ± SD data from experiments in triplicate. *P\0.05 and **P\0.01

    Cell Biochem Biophys, 2016, 74(2):277-83. Imatinib (STI571) purchased from Selleck.

  • Cell Viability assay results. A2C12, BetaD5, GammaA3, GammaD12, A549, CaCo2, HepG2 cell lines were treated with imatinib mesylate for 24h and 96h.

    Dr. Thomas Kruwel of Fraunhofer. Imatinib (STI571) purchased from Selleck.

    A. Viability curve for the c-Kit mutant MelMS melanoma cell line treated with increasing concentrations of imatinib for 72h (relative to DMSO-treated controls; mean ±sd; n=3) B. MelMS melanoma cells were treated with 50nM imatinib for 24h. The effects on c-Kit, ERK and AKT activation were determined by immunoblotting.

    Dr. Helen Rizos from the university of Sydney. Imatinib (STI571) purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Imatinib (STI571) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.
Targets
PDGFR [1]
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
In vitro

In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. [1] Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. [2] Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. [3] A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LAMA-84 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEH6dYFKSzVyPUCuNFc{ODRizszN NWHjNW1SW0GQR1XS
EM-2 Mk\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7RVGVKSzVyPUCuNFg5QCEQvF2= NHvN[JZUSU6JRWK=
MEG-01 MlG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[xUIhQUUN3ME2wMlA5QTJzIN88US=> NVS2UGhnW0GQR1XS
BV-173 MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwMUi3OEDPxE1? MWPTRW5ITVJ?
K-562 Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHNTWM2OD1yLkKyOFMzKM7:TR?= NYDDdWxxW0GQR1XS
CGTH-W-1 M{n6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[5[WFKSzVyPUCuN|g{PzRizszN MkPrV2FPT0WU
ST486 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XTW2lEPTB;MD62PFU1KM7:TR?= M3rLfXNCVkeHUh?=
NCI-H1436 MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXTW3RKSzVyPUCuPVc5ODFizszN M3e2dnNCVkeHUh?=
NOS-1 M2X2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rXNWlEPTB;MT62OVM5OyEQvF2= NIi1T5pUSU6JRWK=
A498 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJwNUeyNlMh|ryP MXnTRW5ITVJ?
BE-13 M2nNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJwNkKxNFYh|ryP MoLGV2FPT0WU
SUP-T1 M162ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4q2WGlEPTB;Mz64NlkxPyEQvF2= NUTqUZNnW0GQR1XS
NCI-H1770 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPq[IlqUUN3ME21MlU4OjZ{IN88US=> Ml;VV2FPT0WU
IMR-5 NYnxNlBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fQZWlEPTB;Nj6yNlE1PyEQvF2= NW[0dpB4W0GQR1XS
LB2241-RCC NWjxTplyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRThwMEezPFQh|ryP NYH3e|NnW0GQR1XS
TGBC24TKB M{HiSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XwfGlEPTB;OD6zOFA2OiEQvF2= M3P4TnNCVkeHUh?=
SCC-15 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\HVXlpUUN3ME2xNE44Pzh6IN88US=> NWXSbnRiW0GQR1XS
BB49-HNC M2rMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrrcIRtUUN3ME2xOE4{OzN3IN88US=> NXzVNmE2W0GQR1XS
ES7 NULLZWhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF2LkezO|kh|ryP MkPMV2FPT0WU
LB2518-MEL MoPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G2NWlEPTB;MU[uOlA6PCEQvF2= Mo\6V2FPT0WU
NCI-H510A MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zaXmlEPTB;MUeuNlQ1OiEQvF2= NF3FVGxUSU6JRWK=
TE-441-T MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;tWJlKSzVyPUG3MlI5QDZizszN NYTlT2FFW0GQR1XS
HH NHTtR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jOe2lEPTB;MUeuN|k6QSEQvF2= NIXtTIpUSU6JRWK=
LC4-1 NWHRVJg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF6LkC2OVIh|ryP M4TZbXNCVkeHUh?=
KARPAS-45 NX64[Gk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPUTWM2OD1zOD6xPFQ5KM7:TR?= NV\OdZRbW0GQR1XS
LB1047-RCC NGOxXmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\jTWM2OD1zOD60OFUzKM7:TR?= NX;EfFY2W0GQR1XS
NKM-1 Mni3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DQU2lEPTB;MUmuN|U2OiEQvF2= MmroV2FPT0WU
SCLC-21H M{TkTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvwTWM2OD1{MD6xNlQ3KM7:TR?= NIDKOnpUSU6JRWK=
RS4-11 Mk[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL5TWM2OD1{MD6zN|A5KM7:TR?= M3nC[HNCVkeHUh?=
ALL-PO MkDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHFTWM2OD1{MD64NVQ6KM7:TR?= MXvTRW5ITVJ?
GDM-1 M124SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDWOFhjUUN3ME2yNk42QTR3IN88US=> M{TqWXNCVkeHUh?=
DMS-79 NWTPfZo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYqxdYFXUUN3ME2yOE41QTN2IN88US=> NF24UZNUSU6JRWK=
MPP-89 MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTJ3Lk[4O|Qh|ryP NXjKdoVOW0GQR1XS
NB10 MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ4LkS2PVkh|ryP M1XkUHNCVkeHUh?=
LS-513 NYCxOpM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fWbGlEPTB;Mk[uPFg1PyEQvF2= NILLfJlUSU6JRWK=
L-540 NEjmXVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJ4LkmxOFMh|ryP NVXLR3RlW0GQR1XS
ES1 NXjOXHAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPRfoZNUUN3ME2yO{42OjFizszN MWjTRW5ITVJ?
NTERA-S-cl-D1 MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfndlB[UUN3ME2zNE42ODl|IN88US=> NILme2NUSU6JRWK=
EW-1 NV;OWWJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1S2SGlEPTB;M{KuPVQ2PCEQvF2= MoDWV2FPT0WU
Calu-6 NYHLb4tTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTN|LkG4OVUh|ryP MoDvV2FPT0WU
CTV-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Gzc2lEPTB;M{OuPVc5QSEQvF2= Mn35V2FPT0WU
YT NH35TpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTN6LkWyNFkh|ryP Mlu1V2FPT0WU
TE-6 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjrTWM2OD12MT6yO|k5KM7:TR?= M3H2fHNCVkeHUh?=
HT-144 NIHtdJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7te41KSzVyPUSxMlU1QDZizszN MV7TRW5ITVJ?
EW-13 NGe1OWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[3XZlKSzVyPUSyMlI4QTFizszN NY\OWZZyW0GQR1XS
KALS-1 NX3GRnlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTR|LkGzNlkh|ryP MlG0V2FPT0WU
MOLT-16 NYTwR3VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3GZ4lKSzVyPUS1MlA4PTJizszN NWL3NIQ6W0GQR1XS
D-336MG MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfZTWM2OD12NT65OVk6KM7:TR?= NHvvUZlUSU6JRWK=
TE-11 NV;JSHBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR4Lk[1N{DPxE1? MWjTRW5ITVJ?
EB2 M17Kemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLPRYp7UUN3ME20Ok43QTlizszN NU\WVYhPW0GQR1XS
SK-N-DZ Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTR6LkC5OlEh|ryP MoLZV2FPT0WU
SW684 M1fxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTR6LkK2PVUh|ryP MoDwV2FPT0WU
EW-18 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR6LkSzPVUh|ryP MkfCV2FPT0WU
RL95-2 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTVyLkC3NUDPxE1? MljkV2FPT0WU
CHP-126 M3n1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH5eWhKSzVyPUWwMlg6ODVizszN M{Wwe3NCVkeHUh?=
NCI-H1395 Mo[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTVzLke4N|Uh|ryP NUTjdo5{W0GQR1XS
TE-15 MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;2TWM2OD13Mj6yOVU3KM7:TR?= NInxO5pUSU6JRWK=
ES4 NEPpOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rNWmlEPTB;NUKuPVc4PSEQvF2= M{Ox[3NCVkeHUh?=
TE-1 NEXzXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLXW4NrUUN3ME21N{46PDV3IN88US=> MnHIV2FPT0WU
SIMA MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v2R2lEPTB;NUeuN|MyOSEQvF2= NYn1dnE3W0GQR1XS
LB647-SCLC Mn76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHxWVVmUUN3ME22OE4yOTh6IN88US=> MnXYV2FPT0WU
KY821 M3\N[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDETWM2OD14ND6yOVUzKM7:TR?= MWjTRW5ITVJ?
LC-2-ad MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTZ3Lke2NFEh|ryP Mo\RV2FPT0WU
KP-N-RT-BM-1 MknYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPYTWM2OD14Nj62N|Y3KM7:TR?= NWDyPYZzW0GQR1XS
SW872 M4rI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTZ5LkSzPFIh|ryP MXLTRW5ITVJ?
ES5 NXPpfoJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTZ5Lk[5Olgh|ryP MWTTRW5ITVJ?
SK-NEP-1 M4PwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfOdGtPUUN3ME22PE4{QDB|IN88US=> MXrTRW5ITVJ?
RPMI-6666 MkHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1KwZmlEPTB;N{GuNFMzKM7:TR?= NEKwfllUSU6JRWK=
UACC-812 M3HuOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7vXHFKSzVyPUexMlE3ODlizszN MV\TRW5ITVJ?
COLO-829 NEi4eZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTjTWM2OD15Mj62PVg4KM7:TR?= NWXXVIl4W0GQR1XS
KP-N-YS MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTd{LkexN|kh|ryP M4HG[HNCVkeHUh?=
GI-1 NEfvUWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NET3PY1KSzVyPUezMlI5PjhizszN MUjTRW5ITVJ?
ETK-1 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjwN3ZKSzVyPUezMlQ6OzJizszN NG[2UJdUSU6JRWK=
LXF-289 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrNTWM2OD15Mz63Nlkh|ryP NFXDVldUSU6JRWK=
CAS-1 NFfBbJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf6ZYM4UUN3ME23N{45QDV5IN88US=> NGrY[XpUSU6JRWK=
EW-22 M2j5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjiRopKSzVyPUe0MlcyOTVizszN NHrkfplUSU6JRWK=
NCI-H2196 Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD4e201UUN3ME23OU43Ozd7IN88US=> MXXTRW5ITVJ?
EoL-1-cell NVn1VJRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfZVJpKSzVyPUixMlY6PjNizszN NV\DPWxYW0GQR1XS
D-247MG MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3wSppNUUN3ME24Nk4xOjR6IN88US=> MULTRW5ITVJ?
Becker NXrrcY92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn6dW9HUUN3ME24Nk4{PDhzIN88US=> NFH5UZFUSU6JRWK=
IST-MEL1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrnTWM2OD16Mj6zOFgzKM7:TR?= MVLTRW5ITVJ?
MDA-MB-134-VI Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTh{LkW5PVYh|ryP Mn3zV2FPT0WU
NCI-H1092 NVnmWGt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTh2LkCxPVch|ryP NGnwZ4lUSU6JRWK=
KINGS-1 M3ra[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TOeGlEPTB;OE[uNVYyQCEQvF2= MkHmV2FPT0WU
HCC2218 NWfSTpNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTh4Lke5NVMh|ryP MkmwV2FPT0WU
GI-ME-N M1LhN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHLdFRIUUN3ME24O{44Pjl7IN88US=> M2DMb3NCVkeHUh?=
AM-38 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf4So5zUUN3ME24PE4{QTV|IN88US=> M1HLT3NCVkeHUh?=
KNS-42 Ml3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTh7LkGwNVgh|ryP M1TE[XNCVkeHUh?=
C8166 M3fYTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTlRlI2UUN3ME24PU43OTJ3IN88US=> MkLUV2FPT0WU
Ramos-2G6-4C10 NETHcm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH1THFKSzVyPUi5Mlg4OTlizszN M3rtWXNCVkeHUh?=
CTB-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTlyLk[zOVch|ryP MYXTRW5ITVJ?
HCE-4 MoTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXLOFZKSzVyPUmxMlE{OzZizszN MYXTRW5ITVJ?
NCI-H526 NI\iU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;2[WJKSzVyPUmyMlQyODNizszN NIS3e21USU6JRWK=
ECC4 M{P1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTl2LkK1OVUh|ryP MknhV2FPT0WU
NCCIT MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfzV2RKSzVyPUm1MlMzQTJizszN MV\TRW5ITVJ?
MZ7-mel M{m2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTl3LkmwOEDPxE1? NWDFN3h[W0GQR1XS
COLO-684 NFX3fmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DVOmlEPTB;OU[uNlM5PSEQvF2= NUnxVGs2W0GQR1XS
SU-DHL-1 NFmxe|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTl4Lkm4OFIh|ryP M2Hq[nNCVkeHUh?=
SF126 NGC1V3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTl5LkWyNVch|ryP NEDXUIZUSU6JRWK=
NMC-G1 MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLrU5pKSzVyPUm4MlQ2PTRizszN MYLTRW5ITVJ?
NB14 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC0WHVKSzVyPUm4MlkzODhizszN MXjTRW5ITVJ?
VA-ES-BJ NH[xO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoD2TWM2OD17OT60NFU3KM7:TR?= MmHjV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. [5] In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. [6]

Protocol

Kinase Assay:

[1]

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PDGF receptor kinase activity:

PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
Cell Research:

[3]

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  • Cell lines: BON-1 cells and NCI-H727 cells
  • Concentrations: ~100 μM
  • Incubation Time: 48 hours
  • Method:

    BON-1 cells and NCI-H727 cells are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 hours (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
  • Formulation: Imatinib is diluted in water.
  • Dosages: 70 or 100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL (8.1 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 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 Information

Molecular Weight 493.6
Formula

C29H31N7O

CAS No. 152459-95-5
Storage powder
in solvent
Synonyms CGP057148B, ST-1571

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00044304 Recruiting Hypereosinophilic Syndrome National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 22, 2002 Phase 2
NCT02644525 Not yet recruiting Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) December 21, 2015 Phase 2
NCT03007147 Not yet recruiting B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|BCR-ABL1 Fusion Protein Expression|Minimal Residual Disease|Philadelphia Chromosome Positive|T Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Childrens Oncology Group|National Cancer Institute (NCI) July 2017 Phase 3
NCT03023046 Not yet recruiting Adult Acute Lymphoblastic Leukemia|Adult Lymphoblastic Lymphoma|CD20 Positive|Philadelphia Chromosome Positive University of Washington|National Cancer Institute (NCI) February 2017 Phase 2
NCT02538926 Not yet recruiting B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T Lymphoblastic Leukemia/Lymphoma|Refractory B Lymphoblastic Lymphoma|Refractory T Lymphoblastic Lymphoma|T Acute Lymphoblastic Leukemia|T Lymphoblastic Lymphoma University of Washington|National Cancer Institute (NCI) January 2017 Phase 2
NCT02924714 Recruiting Gastrointestinal Stromal Tumor Oslo University Hospital January 2017 Phase 2

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

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID