Imatinib Inhibitor CAS No. 152459-95-5

Cat. No.	Name	Size	Price	Add Cart
KI0301	Imatinib	250 mg	$112
KI0301	Imatinib	500 mg	$192

Chemical Characteristic

Product Name	Imatinib
Synonyms	Gleevec; STI571
CAS No.	152459-95-5
Molecular Weight	493.6
Formula	C₂₉H₃₁N₇O
Chemical Name	4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
Smiles	C(=O)(c1ccc(cc1)CN1CCN(CC1)C)Nc1cc(c(cc1)C)Nc1nc(ccn1)c1cnccc1
Chemical Structure
Documents	HPLC MS COA

Biological activities

Imatinib is a 2-phenylaminopyrimidine derivative that functions as a multi-target inhibitor of tyrosine kinase enzymes with IC50 values of 0.6, 0.1 and 0.1 μM for v-Abl, c-kit and PDGFR, respectively. Imatinib (0.01-10 μM) treatment of human vascular smooth muscle cells (vSMC) in the presence of PDGF dose dependently decreases Sulfur-35 Na2SO4 (³⁵S-SO_{4) incorporation into secreted proteoglycans with a maximal inhibition of 66% at 10 μM imatinib, with an IC50 value of approximately 700 nM. The half maximal saturation value for proteoglycans from imatinib treated human vSMC in the presence of PDGF is approximately 0.05 mg/mL compared to 0.02 mg/mL for PDGF treatment alone, indicating a substantial decrease in LDL binding with imatinib treatment.^[1] Imatinib markedly down-regulates herg1 mRNA expression in dose depend manner and the maximal decrease 67.9 % is obtained at 5 μM. ^[2] The amount of imatinib that reduces K562 chronic myelogenous leukemia cells growth to 50% of that in controls (IC50) is 0.14 μM after 72 hours different dose imatinib (0.2, 0.3, 0.5 and 1 μM) contact. ^[3] Furthermore, after treatment with imatinib in K562 cells, necrosis is more pronounced than apoptosis at high concentrations of imatinib (14% for 1 μM imatinib, 20% for 10 μM imatinib, 72 hours contact).^[4] Inhibition of Steel factor (SLF, ligand of c-kit)-induced c-kit autophosphorylation by imatinib is dose dependent, with complete inhibition observed at both 10 and 1.0 μM and c-kit activation is approximately 50% that in SLF-stimulated M-07e cells (a human myeloid leukemia cell line) not treated with inhibitor at an imatinib dose of 0.1 μM. Besides, in M-07e cells, complete inhibition of SLF-dependent activation of MAP kinase occurrs at 10, 1.0, and 0.5 μM concentrations of imatinib and total MAP kinase expression is not altered by treatment with imatinib.^[5] Imatinib (70 or 100 mg/kg per day in 1 or 2 intra-peritoneal injections) inhibits 80%, 40% and 78% growth of SCLC6, SCLC61 and SCLC108 tumors, respectively, however without any significant inhibition of SCLC74 tumor growth.^[6] In high fat fed ApoE^−/− mice, imatinib (40 mg/kg) does not affect body weight and en face staining with Oil red O shows that imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated control when dosed by gavage at 10, 20 and 40 mg/kg, respectively.^[1]}

Protocols

Fresh stock solutions of imatinib (10 mM) are made by dissolving 5 mg imatinib in 1 mL phosphate-buffered saline (PBS).^[5]

References

[1] Ballinger ML, et al. Imatinib inhibits vascular smooth muscle proteoglycan synthesis and reduces LDL binding in vitro and aortic lipid deposition in vivo. J Cell Mol Med. 2010, 14(6B):1408-1418. [2] Zheng F, et al. Imatinib has the potential to exert its antileukemia effects by down-regulating hERG1 K(+) channels in chronic myelogenous leukemia. Med Oncol. 2011. [3] Huguet F, et al. Growth inhibition by STI571 in combination with radiation in human chronic myelogenous leukemia K562 cells. Mol Cancer Ther. 2008, 7(2): 398-406. [4] Okada M, et al. A novel mechanism for imatinib mesylate-induced cell death of BCR-ABL-positive human leukemic cells: caspase-independent, necrosis-like programmed cell death mediated by serine protease activity. Blood. 2004, 103(6): 2299-2307. [5] Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000, 96(3): 925-932. [6] Decaudin D, et al. In vivo efficacy of STI571 in xenografted human small cell lung cancer alone or combined with chemotherapy. Int J Cancer. 2005, 113(5):849-856.

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