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 37 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 NHz0fZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwMEezNFQh|ryP MYHTRW5ITVJ?
EM-2 M2\EN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHycHVKSzVyPUCuNFg5QCEQvF2= M132NHNCVkeHUh?=
MEG-01 M3TqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHKTWM2OD1yLkC4PVIyKM7:TR?= M{\pbHNCVkeHUh?=
BV-173 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH3clRKSzVyPUCuNVg4PCEQvF2= M1LWXnNCVkeHUh?=
K-562 MkTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHKbZZmUUN3ME2wMlIzPDN{IN88US=> M2nsbnNCVkeHUh?=
CGTH-W-1 M1T4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r4NmlEPTB;MD6zPFM4PCEQvF2= NYrxPGdjW0GQR1XS
ST486 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2KzbGlEPTB;MD62PFU1KM7:TR?= MVnTRW5ITVJ?
NCI-H1436 NW[5NmhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfhfY1HUUN3ME2wMlk4QDBzIN88US=> MmnzV2FPT0WU
NOS-1 NUn3[XU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjCV4JKSzVyPUGuOlU{QDNizszN MXfTRW5ITVJ?
A498 NYHtOnFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTJwNUeyNlMh|ryP MXPTRW5ITVJ?
BE-13 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTJwNkKxNFYh|ryP M3HwZnNCVkeHUh?=
SUP-T1 MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3W3VGlEPTB;Mz64NlkxPyEQvF2= NHzaOYdUSU6JRWK=
NCI-H1770 NUjCW4RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;MR2lEPTB;NT61O|I3OiEQvF2= NVTpW2JEW0GQR1XS
IMR-5 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorMTWM2OD14LkKyNVQ4KM7:TR?= MkTVV2FPT0WU
LB2241-RCC NFnKRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRThwMEezPFQh|ryP NHXMXFhUSU6JRWK=
TGBC24TKB M{HMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrJR5VKSzVyPUiuN|QxPTJizszN MV7TRW5ITVJ?
SCC-15 MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnRWGl2UUN3ME2xNE44Pzh6IN88US=> MVLTRW5ITVJ?
BB49-HNC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTF2LkOzN|Uh|ryP NF3S[plUSU6JRWK=
ES7 NYXCcI1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrCNmlKSzVyPUG0Mlc{PzlizszN NF[yTmxUSU6JRWK=
LB2518-MEL M4Cxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLBTWM2OD1zNj62NFk1KM7:TR?= NXnqZoVjW0GQR1XS
NCI-H510A NYTQ[mw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4j3VWlEPTB;MUeuNlQ1OiEQvF2= NHzudI9USU6JRWK=
TE-441-T NYH4XZNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S5WWlEPTB;MUeuNlg5PiEQvF2= MYXTRW5ITVJ?
HH Mo\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi5TWM2OD1zNz6zPVk6KM7:TR?= NFrLVnFUSU6JRWK=
LC4-1 MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF6LkC2OVIh|ryP MVvTRW5ITVJ?
KARPAS-45 NXXVT3ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjPblhKSzVyPUG4MlE5PDhizszN M3LyeHNCVkeHUh?=
LB1047-RCC NXPmOXpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nDSmlEPTB;MUiuOFQ2OiEQvF2= MV\TRW5ITVJ?
NKM-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF7LkO1OVIh|ryP M3H4ZXNCVkeHUh?=
SCLC-21H NWPjZmxjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK0bpdKSzVyPUKwMlEzPDZizszN MULTRW5ITVJ?
RS4-11 NE\LWXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnToTWM2OD1{MD6zN|A5KM7:TR?= M{XNbXNCVkeHUh?=
ALL-PO NWj3NFgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jxbGlEPTB;MkCuPFE1QSEQvF2= NGPLWIFUSU6JRWK=
GDM-1 NIXGSoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ{LkW5OFUh|ryP NIW2OJNUSU6JRWK=
DMS-79 NVrPWJVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJ2LkS5N|Qh|ryP MX\TRW5ITVJ?
MPP-89 M{PiSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO3WppKSzVyPUK1MlY5PzRizszN NUjke|lWW0GQR1XS
NB10 NV;T[ll5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfDXXI6UUN3ME2yOk41Pjl7IN88US=> M2KwOXNCVkeHUh?=
LS-513 M373Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3vU2l[UUN3ME2yOk45QDR5IN88US=> MmnpV2FPT0WU
L-540 M1qzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[wZ4U{UUN3ME2yOk46OTR|IN88US=> M2jOc3NCVkeHUh?=
ES1 NIjCTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnQOmc5UUN3ME2yO{42OjFizszN NXvXZZFIW0GQR1XS
NTERA-S-cl-D1 NVnvPZlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M173VGlEPTB;M{CuOVA6OyEQvF2= M37kOXNCVkeHUh?=
EW-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTN{Lkm0OVQh|ryP M1;WRnNCVkeHUh?=
Calu-6 NYS5TGkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTN|LkG4OVUh|ryP M4TLWXNCVkeHUh?=
CTV-1 MlPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfvdXV1UUN3ME2zN{46Pzh7IN88US=> MVjTRW5ITVJ?
YT Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrFOo9KSzVyPUO4MlUzODlizszN MWPTRW5ITVJ?
TE-6 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj5O5lKSzVyPUSxMlI4QThizszN MVnTRW5ITVJ?
HT-144 NInRflRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3ScW5KSzVyPUSxMlU1QDZizszN Mn3EV2FPT0WU
EW-13 NEnabVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkSzTWM2OD12Mj6yO|kyKM7:TR?= MoKxV2FPT0WU
KALS-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzhTWM2OD12Mz6xN|I6KM7:TR?= NHPSTVdUSU6JRWK=
MOLT-16 NF3aVGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrMOphPUUN3ME20OU4xPzV{IN88US=> NUTP[pJzW0GQR1XS
D-336MG MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke2TWM2OD12NT65OVk6KM7:TR?= NHrsR2dUSU6JRWK=
TE-11 M2XrNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fqVGlEPTB;NE[uOlU{KM7:TR?= MVzTRW5ITVJ?
EB2 NETI[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTwW3h2UUN3ME20Ok43QTlizszN NEf1dHpUSU6JRWK=
SK-N-DZ M4jE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfmTWM2OD12OD6wPVYyKM7:TR?= M{ToXnNCVkeHUh?=
SW684 NILGd|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILpcWZKSzVyPUS4MlI3QTVizszN M2PFZnNCVkeHUh?=
EW-18 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm1NXRKSzVyPUS4MlQ{QTVizszN NF3CdFhUSU6JRWK=
RL95-2 NVqxeI1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\CT2lEPTB;NUCuNFcyKM7:TR?= NV7LWmJ3W0GQR1XS
CHP-126 M16zfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTVyLki5NFUh|ryP MVPTRW5ITVJ?
NCI-H1395 M{HCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[xTWM2OD13MT63PFM2KM7:TR?= NW\NOZNnW0GQR1XS
TE-15 NGrwNnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\ZXJhHUUN3ME21Nk4zPTV4IN88US=> Mm\PV2FPT0WU
ES4 NWTMU3RlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTV{Lkm3O|Uh|ryP NF7QXY5USU6JRWK=
TE-1 M2q2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfyWJpKSzVyPUWzMlk1PTVizszN M4DHWHNCVkeHUh?=
SIMA M4\sZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvn[ZFQUUN3ME21O{4{OzFzIN88US=> MWfTRW5ITVJ?
LB647-SCLC M1rGNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG2TWM2OD14ND6xNVg5KM7:TR?= MVXTRW5ITVJ?
KY821 Mof1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfQTWM2OD14ND6yOVUzKM7:TR?= M3TJU3NCVkeHUh?=
LC-2-ad NVrwbnpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXBWFFKSzVyPU[1Mlc3ODFizszN Mk\NV2FPT0WU
KP-N-RT-BM-1 M2ToW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTZ4Lk[zOlYh|ryP MYrTRW5ITVJ?
SW872 M4f6UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3JVlNKSzVyPU[3MlQ{QDJizszN Ml:zV2FPT0WU
ES5 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPhPWlKSzVyPU[3MlY6PjhizszN NF24bmJUSU6JRWK=
SK-NEP-1 NXf5dpZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrCTWM2OD14OD6zPFA{KM7:TR?= NXPpN|hOW0GQR1XS
RPMI-6666 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTdzLkCzNkDPxE1? NWfzNnV3W0GQR1XS
UACC-812 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3WyZ2lEPTB;N{GuNVYxQSEQvF2= NIfQOIFUSU6JRWK=
COLO-829 M2jYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PKfmlEPTB;N{KuOlk5PyEQvF2= MlzzV2FPT0WU
KP-N-YS NWrOWVFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHZNVlKSzVyPUeyMlcyOzlizszN MlvOV2FPT0WU
GI-1 NYnyUHRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHTb3Y{UUN3ME23N{4zQDZ6IN88US=> NEDjboxUSU6JRWK=
ETK-1 NEf4XWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTd|LkS5N|Ih|ryP NHSxTXVUSU6JRWK=
LXF-289 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH3XXlUUUN3ME23N{44OjlizszN MXPTRW5ITVJ?
CAS-1 NX\pPItUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\vTWM2OD15Mz64PFU4KM7:TR?= MU\TRW5ITVJ?
EW-22 NYTUNWp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PWR2lEPTB;N{SuO|EyPSEQvF2= NVHkV3g3W0GQR1XS
NCI-H2196 MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13ibmlEPTB;N{WuOlM4QSEQvF2= M1TrNnNCVkeHUh?=
EoL-1-cell MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjMT3hCUUN3ME24NU43QTZ|IN88US=> NXLHdo5pW0GQR1XS
D-247MG NGPr[ZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPL[lZSUUN3ME24Nk4xOjR6IN88US=> MWHTRW5ITVJ?
Becker MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi0cG1KSzVyPUiyMlM1QDFizszN NH;pZZRUSU6JRWK=
IST-MEL1 NXT6VlJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fEdGlEPTB;OEKuN|Q5OiEQvF2= M{\KfXNCVkeHUh?=
MDA-MB-134-VI NY\0fllvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zxUGlEPTB;OEKuOVk6PiEQvF2= Moi5V2FPT0WU
NCI-H1092 NVjPd|A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvSd4I3UUN3ME24OE4xOTl5IN88US=> Mki5V2FPT0WU
KINGS-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1O0[2lEPTB;OE[uNVYyQCEQvF2= NGi4RYtUSU6JRWK=
HCC2218 NGDYZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW1TWM2OD16Nj63PVE{KM7:TR?= NIfyOlVUSU6JRWK=
GI-ME-N M1vnSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojQTWM2OD16Nz63Olk6KM7:TR?= NUPUN4lrW0GQR1XS
AM-38 MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTh6LkO5OVMh|ryP M2nSN3NCVkeHUh?=
KNS-42 MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj2ephKSzVyPUi5MlExOThizszN NEG1Z2RUSU6JRWK=
C8166 MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTh7Lk[xNlUh|ryP M1zwNXNCVkeHUh?=
Ramos-2G6-4C10 NUn5VlNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;ZTWM2OD16OT64O|E6KM7:TR?= NUDlXphjW0GQR1XS
CTB-1 NFi4[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTlyLk[zOVch|ryP M{T5N3NCVkeHUh?=
HCE-4 Mm\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3WPVYyUUN3ME25NU4yOzN4IN88US=> NGnETWVUSU6JRWK=
NCI-H526 NELsbHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHhOm8zUUN3ME25Nk41OTB|IN88US=> NHLwT5FUSU6JRWK=
ECC4 M4TMXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrSNYFwUUN3ME25OE4zPTV3IN88US=> NIWxW|VUSU6JRWK=
NCCIT NViwNmFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTl3LkOyPVIh|ryP NIjKbHlUSU6JRWK=
MZ7-mel MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr4TWM2OD17NT65NFQh|ryP MXvTRW5ITVJ?
COLO-684 M2jrUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknpTWM2OD17Nj6yN|g2KM7:TR?= MXnTRW5ITVJ?
SU-DHL-1 NELH[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn4U2ZKSzVyPUm2Mlk5PDJizszN NGrUR4JUSU6JRWK=
SF126 NVewdGhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvNWGlKSzVyPUm3MlUzOTdizszN MV\TRW5ITVJ?
NMC-G1 NHX1cpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rI[WlEPTB;OUiuOFU2PCEQvF2= M4D5WXNCVkeHUh?=
NB14 NXHk[VlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjhbnpKSzVyPUm4MlkzODhizszN M17nXHNCVkeHUh?=
VA-ES-BJ M2rlfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrCd5JKSzVyPUm5MlQxPTZizszN M3:1fnNCVkeHUh?=

... 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 33 mg/mL (66.85 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
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
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
NCT03722420 Not yet recruiting Chronic Myeloid Leukemia Chronic Phase Il-Yang Pharm. Co. Ltd. December 14 2018 Phase 3
NCT03609424 Not yet recruiting Gastrointestinal Stromal Tumors Asan Medical Center|Novartis December 30 2018 Phase 1|Phase 2
NCT03578367 Recruiting CML|Chronic Myelogenous Leukemia|Leukemia Myeloid Chronic|Hematologic Diseases Novartis Pharmaceuticals|Novartis November 12 2018 Phase 2
NCT03674099 Recruiting Multiple Sclerosis Tomas Olsson|The Swedish Research Council|Karolinska Institutet October 1 2018 Phase 2
NCT03639922 Recruiting Acute Ischaemic Stroke Niaz Ahmed|Karolinska Institutet October 1 2018 Phase 3
NCT03688568 Recruiting Neurofibroma Plexiform Indiana University|Food and Drug Administration (FDA) September 1 2018 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:

    Could you please advise whether it is a clear solution for compound dissolved in vehicle 2% DMSO+30% PEG 300+2% Tween 80+ddH2O?

  • Answer:

    For S2475 Imatinib (STI571), it is soluble in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 2mg/ml. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm it in water bath at 45-50C. Then add PEG and Tween. After they mixed well, dilute with water.

  • Question 2:

    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