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

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  • 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 MkfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXBS3dKSzVyPUCuNFc{ODRizszN MlrhV2FPT0WU
EM-2 NV3vcY1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVq4XZFTUUN3ME2wMlA5QDhizszN NEPCOJBUSU6JRWK=
MEG-01 MljyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwMEi5NlEh|ryP Mkm2V2FPT0WU
BV-173 NFTLOZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHGdJVKSzVyPUCuNVg4PCEQvF2= NWDkdnJFW0GQR1XS
K-562 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ix[2lEPTB;MD6yNlQ{OiEQvF2= NUTZbmkzW0GQR1XS
CGTH-W-1 NVPVd2lYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVu0SpN[UUN3ME2wMlM5Ozd2IN88US=> M3zHT3NCVkeHUh?=
ST486 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fOT2lEPTB;MD62PFU1KM7:TR?= MYrTRW5ITVJ?
NCI-H1436 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\DW2lEPTB;MD65O|gxOSEQvF2= MlX3V2FPT0WU
NOS-1 NFzxT5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfhRYF2UUN3ME2xMlY2Ozh|IN88US=> M37K[HNCVkeHUh?=
A498 MknjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHXZ|JKSzVyPUKuOVczOjNizszN MnzGV2FPT0WU
BE-13 NFe2S21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJwNkKxNFYh|ryP NYnrfWVkW0GQR1XS
SUP-T1 M3W5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTNwOEK5NFch|ryP M1WyfXNCVkeHUh?=
NCI-H1770 NHr2TmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTqTWM2OD13LkW3NlYzKM7:TR?= NUm5Z2Y3W0GQR1XS
IMR-5 MmTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTZwMkKxOFch|ryP NFnGOoRUSU6JRWK=
LB2241-RCC Ml[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPfnU{UUN3ME24MlA4Ozh2IN88US=> MXjTRW5ITVJ?
TGBC24TKB Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPSRVY2UUN3ME24MlM1ODV{IN88US=> NU\COJZiW0GQR1XS
SCC-15 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrKTWM2OD1zMD63O|g5KM7:TR?= MnvRV2FPT0WU
BB49-HNC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHNN|hKSzVyPUG0MlM{OzVizszN NYK5XIp5W0GQR1XS
ES7 NX[1e2ttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\FR3NKSzVyPUG0Mlc{PzlizszN NFjVXGZUSU6JRWK=
LB2518-MEL MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rZWWlEPTB;MU[uOlA6PCEQvF2= NH;rV3NUSU6JRWK=
NCI-H510A NVv2PVh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTwTWM2OD1zNz6yOFQzKM7:TR?= NW\pdXJLW0GQR1XS
TE-441-T NFjKVXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3roVWlEPTB;MUeuNlg5PiEQvF2= MUfTRW5ITVJ?
HH NXXYSmpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PYcGlEPTB;MUeuN|k6QSEQvF2= MnO1V2FPT0WU
LC4-1 NHrKRYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\GTWM2OD1zOD6wOlUzKM7:TR?= NG[xbXJUSU6JRWK=
KARPAS-45 MkDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTF6LkG4OFgh|ryP M2\afXNCVkeHUh?=
LB1047-RCC M{nBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTvTWM2OD1zOD60OFUzKM7:TR?= M1KyR3NCVkeHUh?=
NKM-1 NHrwd3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XvSmlEPTB;MUmuN|U2OiEQvF2= NHmyVoRUSU6JRWK=
SCLC-21H MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7ER4FKSzVyPUKwMlEzPDZizszN M{LQNnNCVkeHUh?=
RS4-11 M{nPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPLb4xKSzVyPUKwMlM{ODhizszN MmjCV2FPT0WU
ALL-PO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrCdnRKSzVyPUKwMlgyPDlizszN M4GzW3NCVkeHUh?=
GDM-1 M3PoNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3izdGlEPTB;MkKuOVk1PSEQvF2= NYr0N|llW0GQR1XS
DMS-79 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJ2LkS5N|Qh|ryP NU\TcWRRW0GQR1XS
MPP-89 NELPcJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDTVXF1UUN3ME2yOU43QDd2IN88US=> NImxelVUSU6JRWK=
NB10 M3P4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLTNGhKSzVyPUK2MlQ3QTlizszN NHfIUGtUSU6JRWK=
LS-513 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4q2WWlEPTB;Mk[uPFg1PyEQvF2= MkXlV2FPT0WU
L-540 M3W3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJ4LkmxOFMh|ryP M1PxfXNCVkeHUh?=
ES1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJ5LkWyNUDPxE1? NF7CWWhUSU6JRWK=
NTERA-S-cl-D1 NELhWlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjGTWM2OD1|MD61NFk{KM7:TR?= M{X4NnNCVkeHUh?=
EW-1 M4rnbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nGRWlEPTB;M{KuPVQ2PCEQvF2= MXrTRW5ITVJ?
Calu-6 M1v6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXriXphnUUN3ME2zN{4yQDV3IN88US=> MU\TRW5ITVJ?
CTV-1 M4nQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3UcIxKSzVyPUOzMlk4QDlizszN M1jLfnNCVkeHUh?=
YT M{T4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTN6LkWyNFkh|ryP NHm5T|VUSU6JRWK=
TE-6 MoLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\MU2FKSzVyPUSxMlI4QThizszN NXPyN5BlW0GQR1XS
HT-144 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTRzLkW0PFYh|ryP MVnTRW5ITVJ?
EW-13 MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2WzVWlEPTB;NEKuNlc6OSEQvF2= NXjo[HNjW0GQR1XS
KALS-1 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWq5OnVHUUN3ME20N{4yOzJ7IN88US=> MljtV2FPT0WU
MOLT-16 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rzWWlEPTB;NEWuNFc2OiEQvF2= NWraWXd5W0GQR1XS
D-336MG MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTR3Lkm1PVkh|ryP M1vQOnNCVkeHUh?=
TE-11 NXrkSW9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD1TWM2OD12Nj62OVMh|ryP Mo\2V2FPT0WU
EB2 NG\3ZYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTR4Lk[5PUDPxE1? MV3TRW5ITVJ?
SK-N-DZ NELCTWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX4TWM2OD12OD6wPVYyKM7:TR?= NYC2[ld{W0GQR1XS
SW684 NFv1eJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2noZmlEPTB;NEiuNlY6PSEQvF2= Ml\YV2FPT0WU
EW-18 M133dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTXTWM2OD12OD60N|k2KM7:TR?= Mn;PV2FPT0WU
RL95-2 NVP2em4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGxTI15UUN3ME21NE4xPzFizszN NHLWS3JUSU6JRWK=
CHP-126 M{TPUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PmV2lEPTB;NUCuPFkxPSEQvF2= NYe0OJZuW0GQR1XS
NCI-H1395 MlzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm3bmVKSzVyPUWxMlc5OzVizszN M{jO[3NCVkeHUh?=
TE-15 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTV{LkK1OVYh|ryP NXS0W3MyW0GQR1XS
ES4 NH;n[YJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPNTWM2OD13Mj65O|c2KM7:TR?= NX3EcXhzW0GQR1XS
TE-1 NULWVmpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT5TWM2OD13Mz65OFU2KM7:TR?= M{mxd3NCVkeHUh?=
SIMA NF;sPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTV5LkOzNVEh|ryP MWrTRW5ITVJ?
LB647-SCLC NIe5bVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPEfnZpUUN3ME22OE4yOTh6IN88US=> NWSxcGNkW0GQR1XS
KY821 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInKflhKSzVyPU[0MlI2PTJizszN MojhV2FPT0WU
LC-2-ad NWXLSoVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrzXI5WUUN3ME22OU44PjBzIN88US=> NXnaPXp3W0GQR1XS
KP-N-RT-BM-1 Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTZ4Lk[zOlYh|ryP MYjTRW5ITVJ?
SW872 M17vbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fjOGlEPTB;NkeuOFM5OiEQvF2= M{fQdHNCVkeHUh?=
ES5 MlLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDOTWM2OD14Nz62PVY5KM7:TR?= NE\6TZNUSU6JRWK=
SK-NEP-1 NUXZd2hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHzW2k{UUN3ME22PE4{QDB|IN88US=> MUHTRW5ITVJ?
RPMI-6666 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTdzLkCzNkDPxE1? MonpV2FPT0WU
UACC-812 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\GR2lKSzVyPUexMlE3ODlizszN MkDtV2FPT0WU
COLO-829 MljPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj5TWM2OD15Mj62PVg4KM7:TR?= MWjTRW5ITVJ?
KP-N-YS M4rPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTd{LkexN|kh|ryP MXvTRW5ITVJ?
GI-1 M1H6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTd|LkK4Olgh|ryP NWr6[3Y6W0GQR1XS
ETK-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[xVlRlUUN3ME23N{41QTN{IN88US=> MkDJV2FPT0WU
LXF-289 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DC[GlEPTB;N{OuO|I6KM7:TR?= MnzzV2FPT0WU
CAS-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;sXGt4UUN3ME23N{45QDV5IN88US=> MnLiV2FPT0WU
EW-22 MmG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFW1NmVKSzVyPUe0MlcyOTVizszN NHnXOlVUSU6JRWK=
NCI-H2196 M32yfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT3T4RTUUN3ME23OU43Ozd7IN88US=> NHPKZXFUSU6JRWK=
EoL-1-cell NWn5V4wxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYH2cG1CUUN3ME24NU43QTZ|IN88US=> NEj4WIhUSU6JRWK=
D-247MG NYTkcoVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHyTWM2OD16Mj6wNlQ5KM7:TR?= M2OwWXNCVkeHUh?=
Becker NFLDTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTh{LkO0PFEh|ryP M{D5SHNCVkeHUh?=
IST-MEL1 Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P6dWlEPTB;OEKuN|Q5OiEQvF2= Mn2yV2FPT0WU
MDA-MB-134-VI NEjMWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTh{LkW5PVYh|ryP NWj6dlZuW0GQR1XS
NCI-H1092 NUnx[2NiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTh2LkCxPVch|ryP MX;TRW5ITVJ?
KINGS-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u1VWlEPTB;OE[uNVYyQCEQvF2= NWLnU21ZW0GQR1XS
HCC2218 MmjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPHTWM2OD16Nj63PVE{KM7:TR?= M{Tqd3NCVkeHUh?=
GI-ME-N MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\nRY9TUUN3ME24O{44Pjl7IN88US=> MWTTRW5ITVJ?
AM-38 NGjxOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTh6LkO5OVMh|ryP NGjENlRUSU6JRWK=
KNS-42 NInvUHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHlTWM2OD16OT6xNFE5KM7:TR?= MoHGV2FPT0WU
C8166 M1SyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDl[lFUUUN3ME24PU43OTJ3IN88US=> NEfkZpBUSU6JRWK=
Ramos-2G6-4C10 NGDo[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLmV5pNUUN3ME24PU45PzF7IN88US=> NYLR[|I3W0GQR1XS
CTB-1 M3jxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvkTWM2OD17MD62N|U4KM7:TR?= MUnTRW5ITVJ?
HCE-4 NXHqWZZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3K4fmlEPTB;OUGuNVM{PiEQvF2= M2nWUHNCVkeHUh?=
NCI-H526 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfTTWM2OD17Mj60NVA{KM7:TR?= M{PySXNCVkeHUh?=
ECC4 MkfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTl2LkK1OVUh|ryP NFHXcZJUSU6JRWK=
NCCIT MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXoOWpKSzVyPUm1MlMzQTJizszN NFrjeYJUSU6JRWK=
MZ7-mel NXLxN3NvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi4SmlxUUN3ME25OU46ODRizszN MUXTRW5ITVJ?
COLO-684 MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTl4LkKzPFUh|ryP M4DENnNCVkeHUh?=
SU-DHL-1 NXfQPJlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTl4Lkm4OFIh|ryP MmS2V2FPT0WU
SF126 NITOXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHOR5ZKUUN3ME25O{42OjF5IN88US=> MUDTRW5ITVJ?
NMC-G1 NHnTSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLidop{UUN3ME25PE41PTV2IN88US=> NEPSSnVUSU6JRWK=
NB14 NF3oVIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTl6LkmyNFgh|ryP M2ToN3NCVkeHUh?=
VA-ES-BJ MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C2ZmlEPTB;OUmuOFA2PiEQvF2= M4qwTXNCVkeHUh?=

... 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
2mg/mL

* 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
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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Frequently Asked Questions

  • Question 1:

    What is the difference between S2475 (Imatinib) and S1026 (Imatinib Mesylate)? Are they water soluble?

  • Answer:

    S2475 is free base of Imatinib while S1026 is a solt form of Imatinib. They have exactly the same biological activity but different solubility. S1026 can be dissolved in water, but S2475 is not soluble in water. S2475 can be dissolved in DMSO at up to 3mg/ml.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID