Volasertib (BI 6727)
BI 6727; Volasertib
CAS:755038-65-4
分子式:C34H50N8O3
分子量:618.8126
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品牌 / 纯度 / 包装
Pharmacology
Flavopiridol is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia.
Efficacy
| Animal Model | Administration | Dosage | Formulation | Description |
|---|---|---|---|---|
| HL-60, SUDHL-4, and Nalm/6 mouse xenograft model[1] | bolus IV or intraperitoneal on each of 5 consecutive days | 7.5 mg/kg | sterile 0.9% NaCl solution | Flavopiridol results in growth delay of tumor |
| PRXFI337 and PRXFI369 xenograft mouse model[2] | administered p.o. on days 1-4 and 7-11 | 10 mg/kg/day | / | Flavopiridol effects tumor regression in PRXF1337 and tumor stasis lasting for 4 weeks in PRXF1369 |
| Hct116 xenografts mouse model[3] | i.p. twice a week for a total of five injections | 11 mg/kg | PBS | Flavopiridol results in an increase in tumor growth |
| MKN-74 xenograft mouse model[4] | administered i.p. twice a week, for a total of four injections | 10 mg/kg | PBS | Flavopiridol results in decrease in tumor volume |
| Adult male Sprague-Dawley rats[5] | gavage | 5 mg/kg | water | Flavopiridol inhibits SMC proliferation and neointimal formation |
Pharmacokinetics and Pharmacodynamics
| Species | male, CD2F1 mice [1] | |
|---|---|---|
| Dose | 5 mg/kg | |
| Administration | daily IV injections | |
| T1/2 | 18 min | |
| CL | 31 mL/min/kg | |
Toxicity
To be updtaed.
References
[1] Arguello F, et al. Blood, 1998, 91(7), 2482-2490.
[2] Drees M, et al. Clin Cancer Res, 1997, 3(2), 273-279.
[3] Motwani M, et al. Clin Cancer Res, 2001, 7(12), 4209-4219.
[4] Motwani M, et al. Mol Cancer Ther, 2003, 2(6), 549-555.
[5] Ruef J, et al. Circulation, 1999, 100(6), 659-665.