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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFSxXm1KSzVyPUCuNFc{ODRizszN M33Dd3NCVkeHUh?=
EM-2 M4fMTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3S[5BKSzVyPUCuNFg5QCEQvF2= MmD6V2FPT0WU
MEG-01 NWezeY84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfsUYFFUUN3ME2wMlA5QTJzIN88US=> NGHXcVlUSU6JRWK=
BV-173 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHKOZJKSzVyPUCuNVg4PCEQvF2= M12xSHNCVkeHUh?=
K-562 NVi4RYlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnjTWM2OD1yLkKyOFMzKM7:TR?= NV3jb452W0GQR1XS
CGTH-W-1 M{OzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTLcJJPUUN3ME2wMlM5Ozd2IN88US=> NIDX[mtUSU6JRWK=
ST486 NYG5PJdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTBwNki1OEDPxE1? M4jkTHNCVkeHUh?=
NCI-H1436 NEf6WZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjKc|FHUUN3ME2wMlk4QDBzIN88US=> NVK1Tm9sW0GQR1XS
NOS-1 MoXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH70dHhKSzVyPUGuOlU{QDNizszN MV7TRW5ITVJ?
A498 NE\UNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\sTnNTUUN3ME2yMlU4OjJ|IN88US=> MnWxV2FPT0WU
BE-13 MlKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nOZmlEPTB;Mj62NlExPiEQvF2= Mo\YV2FPT0WU
SUP-T1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlmxTWM2OD1|LkiyPVA4KM7:TR?= MWTTRW5ITVJ?
NCI-H1770 M1P3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz6TWM2OD13LkW3NlYzKM7:TR?= NF7xcoVUSU6JRWK=
IMR-5 M1TjdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;TU|NKSzVyPU[uNlIyPDdizszN MnH1V2FPT0WU
LB2241-RCC NWXjc5hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRThwMEezPFQh|ryP MXHTRW5ITVJ?
TGBC24TKB NH:xfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7HTWM2OD16LkO0NFUzKM7:TR?= MVPTRW5ITVJ?
SCC-15 NFPndXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX3TWM2OD1zMD63O|g5KM7:TR?= M2rQU3NCVkeHUh?=
BB49-HNC NVT3cVZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rjVWlEPTB;MUSuN|M{PSEQvF2= NIXDNnhUSU6JRWK=
ES7 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[4OJNKSzVyPUG0Mlc{PzlizszN NHThcpNUSU6JRWK=
LB2518-MEL Ml;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFG3bpRKSzVyPUG2MlYxQTRizszN NF\6OFNUSU6JRWK=
NCI-H510A MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jWPWlEPTB;MUeuNlQ1OiEQvF2= NXz0[3BoW0GQR1XS
TE-441-T NGj0[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF5LkK4PFYh|ryP NIn2N5NUSU6JRWK=
HH M2jFb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LncGlEPTB;MUeuN|k6QSEQvF2= MnP0V2FPT0WU
LC4-1 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF62SXBKSzVyPUG4MlA3PTJizszN NHnPUllUSU6JRWK=
KARPAS-45 NUn1Zm5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjrTWM2OD1zOD6xPFQ5KM7:TR?= NFLNfJFUSU6JRWK=
LB1047-RCC NF7iS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjQV2NKSzVyPUG4MlQ1PTJizszN NHLmXFdUSU6JRWK=
NKM-1 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF7LkO1OVIh|ryP NW\D[HlZW0GQR1XS
SCLC-21H Mm\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfYTWM2OD1{MD6xNlQ3KM7:TR?= MoTLV2FPT0WU
RS4-11 NIWzVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\GNVVKSzVyPUKwMlM{ODhizszN NUjJOIhrW0GQR1XS
ALL-PO NF3ZdHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml76TWM2OD1{MD64NVQ6KM7:TR?= NFzKSFVUSU6JRWK=
GDM-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTJ{LkW5OFUh|ryP NWL5c|Z6W0GQR1XS
DMS-79 MoDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LCVWlEPTB;MkSuOFk{PCEQvF2= M3TRRXNCVkeHUh?=
MPP-89 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXMTWM2OD1{NT62PFc1KM7:TR?= NEjR[FRUSU6JRWK=
NB10 NIPPXlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLQTGFkUUN3ME2yOk41Pjl7IN88US=> M4P1THNCVkeHUh?=
LS-513 NVv0NmlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\SdGlEPTB;Mk[uPFg1PyEQvF2= NXS4NG5KW0GQR1XS
L-540 NWruOXloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXLV2ZEUUN3ME2yOk46OTR|IN88US=> NWrPbVlJW0GQR1XS
ES1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrjTWM2OD1{Nz61NlEh|ryP NH\4V3lUSU6JRWK=
NTERA-S-cl-D1 NGfiemxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTNyLkWwPVMh|ryP MYjTRW5ITVJ?
EW-1 M3jQNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki1TWM2OD1|Mj65OFU1KM7:TR?= MonIV2FPT0WU
Calu-6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTI[JF5UUN3ME2zN{4yQDV3IN88US=> M1HNRXNCVkeHUh?=
CTV-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTROm1KSzVyPUOzMlk4QDlizszN MnP0V2FPT0WU
YT NYD1ZmZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPKcVhKSzVyPUO4MlUzODlizszN NF7VdFJUSU6JRWK=
TE-6 NUjP[4tvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXrSIhKSzVyPUSxMlI4QThizszN MkKzV2FPT0WU
HT-144 M3fyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r2cGlEPTB;NEGuOVQ5PiEQvF2= MWnTRW5ITVJ?
EW-13 M3XsPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXteWZNUUN3ME20Nk4zPzlzIN88US=> M2HVW3NCVkeHUh?=
KALS-1 NVzSWVZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLCdW1KSzVyPUSzMlE{OjlizszN NUjrRZVmW0GQR1XS
MOLT-16 NY\HPFh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7nSZZKSzVyPUS1MlA4PTJizszN MUHTRW5ITVJ?
D-336MG MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moq5TWM2OD12NT65OVk6KM7:TR?= NYC3W4ZjW0GQR1XS
TE-11 NILhWpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHixZ3lKSzVyPUS2MlY2OyEQvF2= MnvmV2FPT0WU
EB2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrKVXBKSzVyPUS2MlY6QSEQvF2= MXTTRW5ITVJ?
SK-N-DZ NUK3NlV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTR6LkC5OlEh|ryP NVzKUVFmW0GQR1XS
SW684 M3fRZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13KemlEPTB;NEiuNlY6PSEQvF2= M1LJSHNCVkeHUh?=
EW-18 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X2WWlEPTB;NEiuOFM6PSEQvF2= MnXsV2FPT0WU
RL95-2 M4H0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTVyLkC3NUDPxE1? MXXTRW5ITVJ?
CHP-126 NYTHPItTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFiw[mtKSzVyPUWwMlg6ODVizszN MXXTRW5ITVJ?
NCI-H1395 NH7rVmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\yb2RKUUN3ME21NU44QDN3IN88US=> M1myUHNCVkeHUh?=
TE-15 NFTB[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvrfY9yUUN3ME21Nk4zPTV4IN88US=> NI\Gc2xUSU6JRWK=
ES4 NVXSNWFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\nTWM2OD13Mj65O|c2KM7:TR?= M2W1[3NCVkeHUh?=
TE-1 M4TNR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofUTWM2OD13Mz65OFU2KM7:TR?= MYLTRW5ITVJ?
SIMA MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPQR2JHUUN3ME21O{4{OzFzIN88US=> NUXKS2lLW0GQR1XS
LB647-SCLC NYXhUpU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTZ2LkGxPFgh|ryP NEH5XZJUSU6JRWK=
KY821 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ezSWlEPTB;NkSuNlU2OiEQvF2= NF33VWhUSU6JRWK=
LC-2-ad MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEixRXNKSzVyPU[1Mlc3ODFizszN MXHTRW5ITVJ?
KP-N-RT-BM-1 M4j2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTZ4Lk[zOlYh|ryP M1PqXnNCVkeHUh?=
SW872 NVzmZ5N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrRUmplUUN3ME22O{41Ozh{IN88US=> M4LYbHNCVkeHUh?=
ES5 NGPRZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTZ5Lk[5Olgh|ryP Mnr1V2FPT0WU
SK-NEP-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m5XWlEPTB;NkiuN|gxOyEQvF2= MUjTRW5ITVJ?
RPMI-6666 MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDmVZdKSzVyPUexMlA{OiEQvF2= M{HoNXNCVkeHUh?=
UACC-812 NEmyTopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTdzLkG2NFkh|ryP NV\qVWY6W0GQR1XS
COLO-829 NXX3VZhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jPPWlEPTB;N{KuOlk5PyEQvF2= NXO0O2NJW0GQR1XS
KP-N-YS MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvQNVRbUUN3ME23Nk44OTN7IN88US=> MVrTRW5ITVJ?
GI-1 NYG0SVhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnCbGhxUUN3ME23N{4zQDZ6IN88US=> NHf3fpRUSU6JRWK=
ETK-1 NI[xfGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXiRlBKSzVyPUezMlQ6OzJizszN MlLCV2FPT0WU
LXF-289 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nvVWlEPTB;N{OuO|I6KM7:TR?= MkflV2FPT0WU
CAS-1 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDIeZI{UUN3ME23N{45QDV5IN88US=> NX\GVm9TW0GQR1XS
EW-22 M4T3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTd2LkexNVUh|ryP NHvQS25USU6JRWK=
NCI-H2196 NUnHbIVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3zNG5KSzVyPUe1MlY{PzlizszN MmXjV2FPT0WU
EoL-1-cell M3zlO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRThzLk[5OlMh|ryP NW\MU2MyW0GQR1XS
D-247MG M4[z[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTh{LkCyOFgh|ryP NXHqVFZLW0GQR1XS
Becker MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXKc4ppUUN3ME24Nk4{PDhzIN88US=> M1fRRnNCVkeHUh?=
IST-MEL1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLlOVE3UUN3ME24Nk4{PDh{IN88US=> NEfON29USU6JRWK=
MDA-MB-134-VI M1fQZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTh{LkW5PVYh|ryP NV\lUo1CW0GQR1XS
NCI-H1092 NYP6T3hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDFT5dSUUN3ME24OE4xOTl5IN88US=> MnrFV2FPT0WU
KINGS-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTh4LkG2NVgh|ryP NGSxUXVUSU6JRWK=
HCC2218 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnUUXdKSzVyPUi2Mlc6OTNizszN NYr2SZQxW0GQR1XS
GI-ME-N MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzGSGZKSzVyPUi3Mlc3QTlizszN NFHOS21USU6JRWK=
AM-38 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TjNGlEPTB;OEiuN|k2OyEQvF2= MX\TRW5ITVJ?
KNS-42 M1ryR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrNXJpkUUN3ME24PU4yODF6IN88US=> MmPKV2FPT0WU
C8166 M4\ueGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HBTmlEPTB;OEmuOlEzPSEQvF2= NF;vTY5USU6JRWK=
Ramos-2G6-4C10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTCTWM2OD16OT64O|E6KM7:TR?= NV\0cYt{W0GQR1XS
CTB-1 M{D6ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLJdph7UUN3ME25NE43OzV5IN88US=> M2q5cXNCVkeHUh?=
HCE-4 M3Xwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILmW|ZKSzVyPUmxMlE{OzZizszN M3rBRnNCVkeHUh?=
NCI-H526 NXvjN3ZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTl{LkSxNFMh|ryP M1rmV3NCVkeHUh?=
ECC4 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\JV21qUUN3ME25OE4zPTV3IN88US=> NYrMS5F4W0GQR1XS
NCCIT MnjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrIdGJHUUN3ME25OU4{Ojl{IN88US=> M3jhTnNCVkeHUh?=
MZ7-mel MlOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nsR2lEPTB;OUWuPVA1KM7:TR?= Ml3ZV2FPT0WU
COLO-684 M1TXTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvyTWM2OD17Nj6yN|g2KM7:TR?= NG[we|RUSU6JRWK=
SU-DHL-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzxTWM2OD17Nj65PFQzKM7:TR?= NG[yWVhUSU6JRWK=
SF126 MlnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXGwRm9oUUN3ME25O{42OjF5IN88US=> M4fhdXNCVkeHUh?=
NMC-G1 NW\ReFJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTl6LkS1OVQh|ryP M1Hwc3NCVkeHUh?=
NB14 NIjCOWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrINXlKSzVyPUm4MlkzODhizszN M136XnNCVkeHUh?=
VA-ES-BJ MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrY[WJKSzVyPUm5MlQxPTZizszN NWrnT5d1W0GQR1XS

... 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