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 MlXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULDd2d4UUN3ME2wMlA4OzB2IN88US=> MV7TRW5ITVJ?
EM-2 NUTWW|NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmzTWM2OD1yLkC4PFgh|ryP NImxbItUSU6JRWK=
MEG-01 NFXqfXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq5d2F5UUN3ME2wMlA5QTJzIN88US=> NXzoSIlYW0GQR1XS
BV-173 NWXpTYlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTBOItqUUN3ME2wMlE5PzRizszN MWHTRW5ITVJ?
K-562 NIjIZ4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfWeY9TUUN3ME2wMlIzPDN{IN88US=> NVO5THhLW0GQR1XS
CGTH-W-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zzVGlEPTB;MD6zPFM4PCEQvF2= M{S5U3NCVkeHUh?=
ST486 NYfQWJozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvpdpE1UUN3ME2wMlY5PTRizszN Mkj3V2FPT0WU
NCI-H1436 M{TiR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYCzT3Z{UUN3ME2wMlk4QDBzIN88US=> NEjXXWZUSU6JRWK=
NOS-1 NXXBdHhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGf4fmxKSzVyPUGuOlU{QDNizszN MVHTRW5ITVJ?
A498 NH3JZoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\SNmlEPTB;Mj61O|IzOyEQvF2= NUfpNWJKW0GQR1XS
BE-13 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PFXWlEPTB;Mj62NlExPiEQvF2= MYDTRW5ITVJ?
SUP-T1 NYHSWFRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDNSVhEUUN3ME2zMlgzQTB5IN88US=> NH32dZdUSU6JRWK=
NCI-H1770 NVTYVoVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f6VmlEPTB;NT61O|I3OiEQvF2= MkXOV2FPT0WU
IMR-5 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTZwMkKxOFch|ryP MXfTRW5ITVJ?
LB2241-RCC NXS1eYtrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRThwMEezPFQh|ryP MYfTRW5ITVJ?
TGBC24TKB MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXhS5VoUUN3ME24MlM1ODV{IN88US=> M2qyTnNCVkeHUh?=
SCC-15 M4Tubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfTN45KSzVyPUGwMlc4QDhizszN MknrV2FPT0WU
BB49-HNC MmT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLIbWk5UUN3ME2xOE4{OzN3IN88US=> M2HNfXNCVkeHUh?=
ES7 NHTlV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF2LkezO|kh|ryP MmLCV2FPT0WU
LB2518-MEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\2RWlEPTB;MU[uOlA6PCEQvF2= NEf3U3FUSU6JRWK=
NCI-H510A Mn3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF5LkK0OFIh|ryP NV2ySXVLW0GQR1XS
TE-441-T NGq3NmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTF5LkK4PFYh|ryP NVv6PWlWW0GQR1XS
HH MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy5ZWJKSzVyPUG3MlM6QTlizszN NXn2RVBQW0GQR1XS
LC4-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33yNmlEPTB;MUiuNFY2OiEQvF2= NHS4d4dUSU6JRWK=
KARPAS-45 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT1dGJqUUN3ME2xPE4yQDR6IN88US=> MUjTRW5ITVJ?
LB1047-RCC Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jzVmlEPTB;MUiuOFQ2OiEQvF2= M1rVc3NCVkeHUh?=
NKM-1 MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7JTWM2OD1zOT6zOVUzKM7:TR?= M1jmc3NCVkeHUh?=
SCLC-21H MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPsV|ZKSzVyPUKwMlEzPDZizszN M3fpV3NCVkeHUh?=
RS4-11 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIG4cJRKSzVyPUKwMlM{ODhizszN NHvRXlRUSU6JRWK=
ALL-PO MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlOwTWM2OD1{MD64NVQ6KM7:TR?= MUnTRW5ITVJ?
GDM-1 NYPNeY5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHDT25KSzVyPUKyMlU6PDVizszN NG\zPWlUSU6JRWK=
DMS-79 NX;kZVM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[3XnptUUN3ME2yOE41QTN2IN88US=> MXvTRW5ITVJ?
MPP-89 Mn[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJ3Lk[4O|Qh|ryP NIPScJJUSU6JRWK=
NB10 M4m5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJ4LkS2PVkh|ryP MmnJV2FPT0WU
LS-513 MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnLeZRKSzVyPUK2Mlg5PDdizszN Ml;NV2FPT0WU
L-540 M2HCe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PkPWlEPTB;Mk[uPVE1OyEQvF2= MWXTRW5ITVJ?
ES1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\uOWlEPTB;MkeuOVIyKM7:TR?= Mln3V2FPT0WU
NTERA-S-cl-D1 MnHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULoZVhFUUN3ME2zNE42ODl|IN88US=> NF\3bWdUSU6JRWK=
EW-1 MlfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvOUW1PUUN3ME2zNk46PDV2IN88US=> M4ewd3NCVkeHUh?=
Calu-6 Mny5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjJdmJEUUN3ME2zN{4yQDV3IN88US=> M4q2NXNCVkeHUh?=
CTV-1 NHfyOYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XPNmlEPTB;M{OuPVc5QSEQvF2= MmnyV2FPT0WU
YT MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\3b4JKSzVyPUO4MlUzODlizszN MmOwV2FPT0WU
TE-6 NV\mbpZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzPTWM2OD12MT6yO|k5KM7:TR?= MnTtV2FPT0WU
HT-144 NUTxSldWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHIO3NKSzVyPUSxMlU1QDZizszN M3jtWnNCVkeHUh?=
EW-13 MlLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHZfIFKSzVyPUSyMlI4QTFizszN NWDa[4ZtW0GQR1XS
KALS-1 M3LZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTR|LkGzNlkh|ryP MVfTRW5ITVJ?
MOLT-16 NWD5V5NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXX4OXE{UUN3ME20OU4xPzV{IN88US=> NFLqPXdUSU6JRWK=
D-336MG MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rGT2lEPTB;NEWuPVU6QSEQvF2= M{S2VXNCVkeHUh?=
TE-11 NX2z[mFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGK4ZopKSzVyPUS2MlY2OyEQvF2= MY\TRW5ITVJ?
EB2 M1vS[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvzTWM2OD12Nj62PVkh|ryP M3PMfHNCVkeHUh?=
SK-N-DZ NHzPU|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTndWJWUUN3ME20PE4xQTZzIN88US=> MorxV2FPT0WU
SW684 MnnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfhTWZKSzVyPUS4MlI3QTVizszN NYL3cpBFW0GQR1XS
EW-18 NGDmeG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXxeXNKSzVyPUS4MlQ{QTVizszN NYnvPGNVW0GQR1XS
RL95-2 M4DOPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XTXmlEPTB;NUCuNFcyKM7:TR?= NXTjZnBZW0GQR1XS
CHP-126 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml36TWM2OD13MD64PVA2KM7:TR?= NVXRNFBXW0GQR1XS
NCI-H1395 M1TtZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jhbWlEPTB;NUGuO|g{PSEQvF2= NWHR[o1FW0GQR1XS
TE-15 NXzyTFViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrKTWM2OD13Mj6yOVU3KM7:TR?= NWfzdFRVW0GQR1XS
ES4 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT3TWM2OD13Mj65O|c2KM7:TR?= MVXTRW5ITVJ?
TE-1 M2GxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNUmlEPTB;NUOuPVQ2PSEQvF2= MUHTRW5ITVJ?
SIMA MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTV5LkOzNVEh|ryP MmfDV2FPT0WU
LB647-SCLC MlvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTZ2LkGxPFgh|ryP NGHQcW9USU6JRWK=
KY821 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfYWG5KSzVyPU[0MlI2PTJizszN NGjuO3NUSU6JRWK=
LC-2-ad Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;OTWM2OD14NT63OlAyKM7:TR?= NXTRWXJHW0GQR1XS
KP-N-RT-BM-1 NH76dWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zBemlEPTB;Nk[uOlM3PiEQvF2= Moj6V2FPT0WU
SW872 NYPkXIpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK5TWM2OD14Nz60N|gzKM7:TR?= M33ycXNCVkeHUh?=
ES5 NV:4RXlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrGWY1KSzVyPU[3MlY6PjhizszN NIfZRXhUSU6JRWK=
SK-NEP-1 NEC0UJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTZ6LkO4NFMh|ryP NEPiVXVUSU6JRWK=
RPMI-6666 NFXEXFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTdzLkCzNkDPxE1? M1HHeXNCVkeHUh?=
UACC-812 M1ewW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED4ZW9KSzVyPUexMlE3ODlizszN MUjTRW5ITVJ?
COLO-829 M2S0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTd{Lk[5PFch|ryP M{XRVHNCVkeHUh?=
KP-N-YS MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUX4R4RJUUN3ME23Nk44OTN7IN88US=> Mnq5V2FPT0WU
GI-1 NFXXUXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rnbWlEPTB;N{OuNlg3QCEQvF2= M3zDVHNCVkeHUh?=
ETK-1 NEDnRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULXSldyUUN3ME23N{41QTN{IN88US=> NHvyVVhUSU6JRWK=
LXF-289 M3;OXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTpPXpCUUN3ME23N{44OjlizszN M2O2OXNCVkeHUh?=
CAS-1 NGfxOpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nEWWlEPTB;N{OuPFg2PyEQvF2= MXHTRW5ITVJ?
EW-22 NEm5cnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLwTWM2OD15ND63NVE2KM7:TR?= NFzQeY1USU6JRWK=
NCI-H2196 NWfPSnM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrpOGxKSzVyPUe1MlY{PzlizszN NX[yVXFqW0GQR1XS
EoL-1-cell NVvLcJZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PzTmlEPTB;OEGuOlk3OyEQvF2= NI\aSW9USU6JRWK=
D-247MG M4jtcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTh{LkCyOFgh|ryP NGnkUGlUSU6JRWK=
Becker MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnJUINuUUN3ME24Nk4{PDhzIN88US=> MlPvV2FPT0WU
IST-MEL1 M3PMVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknsTWM2OD16Mj6zOFgzKM7:TR?= MULTRW5ITVJ?
MDA-MB-134-VI NU\VdpdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS5TWM2OD16Mj61PVk3KM7:TR?= M1vaV3NCVkeHUh?=
NCI-H1092 M2rjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki0TWM2OD16ND6wNVk4KM7:TR?= NW\BOXFuW0GQR1XS
KINGS-1 NHTGOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTh4LkG2NVgh|ryP NHnTe|BUSU6JRWK=
HCC2218 MoHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnLT3RFUUN3ME24Ok44QTF|IN88US=> M1:1cnNCVkeHUh?=
GI-ME-N MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nlfGlEPTB;OEeuO|Y6QSEQvF2= Mm\3V2FPT0WU
AM-38 NFHKc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfoTWM2OD16OD6zPVU{KM7:TR?= MkXvV2FPT0WU
KNS-42 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTh7LkGwNVgh|ryP NVnYUo9rW0GQR1XS
C8166 NGPmSG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTh7Lk[xNlUh|ryP NHjEOZNUSU6JRWK=
Ramos-2G6-4C10 Mln3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL4TWM2OD16OT64O|E6KM7:TR?= MWLTRW5ITVJ?
CTB-1 MkH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\NTWM2OD17MD62N|U4KM7:TR?= M2PnZ3NCVkeHUh?=
HCE-4 M2rFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTZNINKSzVyPUmxMlE{OzZizszN NGTuU49USU6JRWK=
NCI-H526 NUTWcmV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTl{LkSxNFMh|ryP MWnTRW5ITVJ?
ECC4 MnXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTl2LkK1OVUh|ryP NWX2fVBTW0GQR1XS
NCCIT NH\jT5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{O3SGlEPTB;OUWuN|I6OiEQvF2= NFW1OlhUSU6JRWK=
MZ7-mel MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DsWGlEPTB;OUWuPVA1KM7:TR?= NGnhS4pUSU6JRWK=
COLO-684 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofFTWM2OD17Nj6yN|g2KM7:TR?= NYPkR4d1W0GQR1XS
SU-DHL-1 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHHTWM2OD17Nj65PFQzKM7:TR?= NVjETIlkW0GQR1XS
SF126 M17wdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLWZ3pjUUN3ME25O{42OjF5IN88US=> MmX1V2FPT0WU
NMC-G1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTl6LkS1OVQh|ryP MlPUV2FPT0WU
NB14 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLBTWM2OD17OD65NlA5KM7:TR?= NEL2VpRUSU6JRWK=
VA-ES-BJ NHn6boVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHuTWM2OD17OT60NFU3KM7:TR?= NWTpUplkW0GQR1XS

... 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]

+ Expand

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:
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
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:

    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