Imatinib

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Chemical Structure| 152459-95-5 同义名 : STI571; CGP-57148B
CAS号 : 152459-95-5
货号 : A150400
分子式 : C29H31N7O
纯度 : 98%
分子量 : 493.6
MDL号 : MFCD05662257
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(24.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • PDGFR

    PDGFR, IC50:100 nM
描述 Imatinib is a multiple target inhibitor with IC50 values of 100nM, 100nM, 38nM, 25nM and 25nM for PDGFR, c-kit, v-Abl, c-abl and bcr-abl (measured by in vitro enzyme assays), respectively, usually used for treatment of chronic myelogenous leukemia (CML)[1][2][3]. In cellular study showed that treatment with Imatinib for 90min could selectively inhibited the autophosphorylation of v-AbI at concentration>3μM in PB-3c cI. 15 cells, PDGF-BB-induced autophosphorylation of PDGFR at concentration>0.3μM in BALB/c 313 cells[1], steel factor–dependent phosphorylation of c-kit and steel factor-dependent activation of Akt at concentration>1μM in M-07e cells, as well as autophosphorylation of an activated mutant form of c-kit and c-kit–dependent activation of MAP kinase/AKT at concentration>0.1μM in HMC-1 cells. Consistent with this, Imatinib showed anti- proliferative effect on HMC-1 cells by 90%-95% at concentration ranging in 0.1μM-10μM, which may due to the abrogation by Imatinib of antiapoptotic effect of mutant c-kit activation. [2]. Intraperitoneal injection with Imatinib at dose of 50mg/kg once daily for 30 days suppressed tumor growth in BALB/c AMuLV and BALB/c 3T3 v-sis cells xenograft mice[1].
作用机制 Imatinib can bind with the ATP binding site of BCR/ABL tyrosine kinase, thus keeps BCR/ABL in an inactive form[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
A498 Growth Inhibition Assay IC50=2.57223 μM SANGER
ALL-PO Growth Inhibition Assay IC50=20.8149 μM SANGER
AM-38 Growth Inhibition Assay IC50=88.3953 μM SANGER
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01400074 Chronic Myeloid Leukemia Phase 3 Unknown June 2014 Korea, Republic of ... 展开 >> Seoul St. Mary's Hospital Recruiting Seoul, Korea, Republic of, 137-701 收起 <<
NCT01083589 Non-small Cell Lung Cancer Phase 2 Completed - United States, Texas ... 展开 >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00154349 Philadelphia Chromosome Positi... 展开 >>ve Acute Lymphocytic Leukemia 收起 << Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.13mL

2.03mL

1.01mL

20.26mL

4.05mL

2.03mL
参考文献

[1]Buchdunger E, Zimmermann J, et al. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res. 1996 Jan 1;56(1):100-4.

[2]Heinrich MC, Griffith DJ, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.

[3]Druker BJ, Tamura S, et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med. 1996 May;2(5):561-6.

[4]Marcucci G, Perrotti D, et al. Understanding the molecular basis of imatinib mesylate therapy in chronic myelogenous leukemia and the related mechanisms of resistance. Commentary re: A. N. Mohamed et al., The effect of imatinib mesylate on patients with Philadelphia chromosome-positive chronic myeloid leukemia with secondary chromosomal aberrations. Clin. Cancer Res., 9: 1333-1337, 2003. Clin Cancer Res. 2003 Apr;9(4):1248-52.