[CAS NO. 152459-95-5] Imatinib (STI571)

Name: Imatinib (STI571)
Brand: Arctom Scientific
SKU: SLK-S2475

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PRODUCTS SPECIFICATIONS [152459-95-5]

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Catalog

SLK-S2475

Brand

Selleck

CAS

152459-95-5

DESCRIPTION [152459-95-5]

Overview

MDL	MFCD05662257
Molecular Weight	493.6
Molecular Formula	C29H31N7O
SMILES	N(C=1N=C(C=CN1)C=2C=CC=NC2)C3=CC(NC(=O)C4=CC=C(CN5CCN(C)CC5)C=C4)=CC=C3C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0259 mL	10.1297 mL	20.2593 mL
5 mM	0.4052 mL	2.0259 mL	4.0519 mL
10 mM	0.2026 mL	1.0130 mL	2.0259 mL
50 mM	0.0405 mL	0.2026 mL	0.4052 mL

Description

Imatinib (STI571,Gleevec, Glivec, CGP057148B) is a multi-target inhibitor of with inhibition for , and , IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces .

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. 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. 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. 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.

References

[1] Buchdunger E, et al. Proc Natl Acad Sci USA. 1995, 92(7), 2558–2562.
[2] Heinrich MC, et al. Blood. 2000, 96(3), 925-932.
[3] Yao JC, et al. Clin Cancer Res. 2007, 13(1), 234-240.
[4] Zheng F, et al. Med Oncol, 2012, 29(3), 2127-2135.
[5] Decaudin D, et al. Int J Cancer. 2005, 113(5), 849-856.
[6] Ballinger ML, et al. J Cell Mol Med. 2010,14(6B), 1408-1418.

Synonyms

Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-

4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide

CGP 57148

Imatinib

4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino]phenyl]benzamide

Genfatinib

N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide