产品
编 号：F284275
分子式：C31H33F3N6O3
分子量：594.63
分子式：C31H33F3N6O3
分子量：594.63
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CAS No: 2304344-56-5
产品详情
生物活性：
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.
体内研究：
CHMFL-ABL-039 (25-100 mg/kg; given i.p.injection; daily for 28 days in K562 mediated five weeks old female nu/nu mice models, daily for 11 days in BaF3-BCR-ABL-V299L mediated five weeks old female nu/nu mice models) do not exhibit any apparent general toxicity and do not affect the mouse weight. CHMFL-ABL-039 can dose dependently suppress the tumor progression for both models at either dosage.Animal Model:BaF3-BCR-ABL-V299L (Imatinib insensitive) and K562 cells inoculated xenograft mouse model (Five weeks old female nu/nu mice)
Dosage:25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:Given i.p.injection; daily for 28 days (K562 mediated models), daily for 11 days (BaF3-BCR-ABL-V299L mediated models)
Result:Did not exhibit any apparent general toxicity and did not affect the mouse weight. Dose dependently suppressed the tumor progression for both models at the dosage of 25, 50 and 100 mg/kg.25 mg/kg daily administration of CHMFL-ABL-039 could achieve 77% tumor growth inhibition (TGI) in K562 mediated models and 100 mg/kg dosage even almost completely eliminated the tumor (TGI: about 100%). In the Imatinib insensitive BaF3- BCR-ABL-V299L mutant cells mediated xenograft model, 25 mg/kg dosage of CHMFL-ABL-039 displayed similar efficacy as 100 mg/kg.
体外研究：
CHMFL-ABL-039 (0-10 μM; 72 hours) is 6-10 fold more sensitive than Imatinib to BCRABL driven cancer cell lines, and BCR-ABL independent cell lines display a great selectivity window comparing to BCRABL driven cancer cell lines. CHMFL-ABL-039 exhibits no general cytotoxicity.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 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.
体内研究：
CHMFL-ABL-039 (25-100 mg/kg; given i.p.injection; daily for 28 days in K562 mediated five weeks old female nu/nu mice models, daily for 11 days in BaF3-BCR-ABL-V299L mediated five weeks old female nu/nu mice models) do not exhibit any apparent general toxicity and do not affect the mouse weight. CHMFL-ABL-039 can dose dependently suppress the tumor progression for both models at either dosage.Animal Model:BaF3-BCR-ABL-V299L (Imatinib insensitive) and K562 cells inoculated xenograft mouse model (Five weeks old female nu/nu mice)
Dosage:25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:Given i.p.injection; daily for 28 days (K562 mediated models), daily for 11 days (BaF3-BCR-ABL-V299L mediated models)
Result:Did not exhibit any apparent general toxicity and did not affect the mouse weight. Dose dependently suppressed the tumor progression for both models at the dosage of 25, 50 and 100 mg/kg.25 mg/kg daily administration of CHMFL-ABL-039 could achieve 77% tumor growth inhibition (TGI) in K562 mediated models and 100 mg/kg dosage even almost completely eliminated the tumor (TGI: about 100%). In the Imatinib insensitive BaF3- BCR-ABL-V299L mutant cells mediated xenograft model, 25 mg/kg dosage of CHMFL-ABL-039 displayed similar efficacy as 100 mg/kg.
体外研究：
CHMFL-ABL-039 (0-10 μM; 72 hours) is 6-10 fold more sensitive than Imatinib to BCRABL driven cancer cell lines, and BCR-ABL independent cell lines display a great selectivity window comparing to BCRABL driven cancer cell lines. CHMFL-ABL-039 exhibits no general cytotoxicity.CHMFL-ABL-039 (0.01-3 μM; 4 hours) can dose dependently inhibit the ABL Y245 phosphorylation and the subsequent downstream signaling mediators.
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