S81023 |
Bafetinib (INNO-406) |
MedMol | 96% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.
- 靶點: Autophagy;Bcr-Abl;Src;Others
- 體內(nèi)研究:
In Bcr-Abl–positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. [1] In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and cyclosporine A (CsA) (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone
- 細(xì)胞實驗: K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells are plated at 1 × 103 in 96-well plates, whereas KU812 and U937 cells are plated at 5 × 103 in 96-well plates. Cells are incubated with serial dilutions of Bafetinib for 3 days. Cell proliferation is measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Nacalai Tesque) assay, and the 50% inhibitory concentration (IC50) values are calculated by fitting the data to a logistic curve. (Only for Reference)
- 參考文獻(xiàn):
1.Kimura S, et al. Blood. 2005, 106(12), 3948-3954. 2.Jing Y, Dai X, Yang L, et al. STING couples with PI3K to regulate actin reorganization during BCR activation[J]. Science Advances. 2020, 6(17): eaax9455. 3.Kamitsuji Y, et al. Cell Death Differ. 2008, 15(11), 1712-2172. 4.Yokota A, et al. Blood. 2007, 109(1), 306-314.
- 溶解性: Ethanol:<1 mg/mL DMSO:93 mg/mL (161.3 mM) H2O:<1 mg/mL
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.734 ml 8.671 ml 17.342 ml 5 mM 0.347 ml 1.734 ml 3.468 ml 10 mM 0.173 ml 0.867 ml 1.734 ml 50 mM 0.035 ml 0.173 ml 0.347 ml
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輸入產(chǎn)品批號:
本計算器可幫助您計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)