S80026 |
DCC-2036 (Rebastinib) |
源葉(MedMol) | 99% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
- 靶點(diǎn): IC50: 0.75±0.11 nM (ABL1WT), 2±0.3 nM (FLT3), 4±0.3 nM (KDR), 6±0.3 nM (TIE2), 34±6 nM (SRC);Apoptosis;FLT;Bcr-Abl;Src
- 體內(nèi)研究:
A single dose of Rebastinib (DCC-2036; oral; 100 mg/kg) affords circulating plasma levels that exceeds 12 μM for up to 24 hours, and effectively inhibits BCR-ABL1 signaling for up to 8 hours in Ba/F3-BCR-ABL1T315I leukemia cells isolated from BM and spleen of tumor-bearing mice. Treatment of mice bearing Ba/F3-BCR-ABL1T315I leukemia cells with Rebastinib at 100 mg/kg once daily by oral gavage significantly prolonged their survival, while STI571 at 100 mg/kg twice daily is ineffective. In this aggressive allograft model, Rebastinib is as effective for treatment of BCR-ABLT315I leukemia as STI571 at 100 mg/kg twice daily in BCR-ABL1native leukemia, and reduces the leukemia cell burden in the spleens of treated mice.
- 參考文獻(xiàn):
1. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011, 19(4), 556-568.
- 溶解性: DMSO : 50 mg/mL (90.32 mM; ultrasonic and warming and heat to 80°C)
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.806 ml 9.032 ml 18.064 ml 5 mM 0.361 ml 1.806 ml 3.613 ml 10 mM 0.181 ml 0.903 ml 1.806 ml 50 mM 0.036 ml 0.181 ml 0.361 ml
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輸入產(chǎn)品批號:
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)