CHMFL-ABL-039 是一种具有高效选择性的 Ⅱ 型野生型 ABL 激酶和耐药 V299L 突变型 Bcr-Abl 激酶的抑制剂,IC50 分别为 7.9 nM、27.9 nM。CHMFL-ABL-039 可用于慢性粒细胞白血病 (CML) 的研究。
产品描述
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor (IC50s: 7.9 nM and 27.9 nM) used in the research of chronic myeloid leukemia.
体外活性
CHMFL-ABL-039 (0.01-3 μM; 4 hours) can dose-dependently inhibit the ABL Y245 phosphorylation and the subsequent downstream signaling mediators. CHMFL-ABL-039 (0-10 μM; 72 hours) is 6-10 fold more sensitive than Imatinib to BCR-ABL driven cancer cell lines, and BCR-ABL independent cell lines display a great selectivity window comparing to BCR-ABL driven cancer cell lines[1].
体内活性
CHMFL-ABL-039 (0.01-3 μM; 4 hours) can dose-dependently inhibit the ABL Y245 phosphorylation and the subsequent downstream signaling mediators. CHMFL-ABL-039 (0-10 μM; 72 hours) is 6-10 fold more sensitive than Imatinib to BCR-ABL drove cancer cell lines, and BCR-ABL independent cell lines display a great selectivity window comparing to BCR-ABL drove cancer cell lines[1].
Cas No.
2304344-56-5
分子式
C31H33F3N6O3
分子量
594.63
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years