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CHMFL-ABL-053 Sale

目录号 : GC17294

CHMFL-ABL-053 (Compound 18a) 是一种有效的、选择性的、可口服的 BCR-ABL、SRC 和 p38 激酶抑制剂,对 ABL1、SRC 和 p38 的 IC50 值分别为 70、90 和 62 nM。

CHMFL-ABL-053 Chemical Structure

Cas No.:1808287-83-3

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5mg
¥2,531.00
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25mg
¥9,188.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

CHMFL-ABL-053 (compound 18a) is a BCR-ABL inhibitor with ABL1: IC50 of 70 nM. CHMFL-ABL-053 is derived from a dihydropyrimidopyrimidine core scaffold based compound 27 (GNF 7). [1]

CHMFL-ABL-053 inhibited the proliferation of CML cell lines K562 (GI50 = 14 nM), KU812 (GI50 = 25 nM) and MEG 01 (GI50 = 16 nM), through significant suppression of the BCR-ABL auto phosphorylation (EC50 = 100 nM) and downstream mediators such as STAT5, Crkl and ERK's phosphorylation. In the TEL fused isogenic BaF3 cells, CHMFL-ABL-053 exhibited strong binding ability against BLK, DDR1, DDR2, EPHA8, EphB6, HCK, LCK, p38α and SRC kinases. CHMFL-ABL-053 exhibited an IC50 of 70 nM against ABL1 kinase, inhibited p38α (IC50: 62 nM) and SRC kinase (IC50: 90 nM) by Invitrogen Select Screen biochemical assay. CHMFL-ABL-053 showed less potent to DDR1 (IC50: 292 nM) and DDR2 (IC50: 457 nM). CHMFL-ABL-053 did not exhibit apparent potency against c-KIT kinase (IC50: over 10000 nM). [1]

Pharmacokinetic study showed that CHMFL-ABL-053 had over 4 hours half-life and 24% bioavailability in rats. 50mg/kg/day dosage treatment could almost completely suppress the tumor progression in the K562 cells inoculated xenograft mouse model. As a potential useful drug candidate for CML, 18a is under extensive preclinical safety evaluation now. [1]

 

Reference:

1.Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl) benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.J Med Chem. 2016 Feb 5. [Epub ahead of print]

Chemical Properties

Cas No. 1808287-83-3 SDF
化学名 2-((3-amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide
Canonical SMILES CC1=CC=C(NC2=NC(NC)=C(C(NC3=CC(NC(C4=CC=CC(C(F)(F)F)=C4)=O)=CC=C3C)=O)C=N2)C=C1N
分子式 C28H26F3N7O2 分子量 549.55
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.8197 mL 9.0984 mL 18.1967 mL
5 mM 0.3639 mL 1.8197 mL 3.6393 mL
10 mM 0.182 mL 0.9098 mL 1.8197 mL
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