S80285 |
Dubermatinib |
源葉(MedMol) | 98% |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.938 ml | 9.689 ml | 19.378 ml |
5 mM | 0.388 ml | 1.938 ml | 3.876 ml |
10 mM | 0.194 ml | 0.969 ml | 1.938 ml |
50 mM | 0.039 ml | 0.194 ml | 0.388 ml |
- 提示:詳情請下載說明書。
- 產品描述: TP-0903 is a potent and selective Axl kinase inhibitor.
- 靶點: Apoptosis;TAM Receptor;Apoptosis;TAMReceptor
- 體外研究:
In pancreatic cancer cells (PSN-1), TP-0903 shows strong antiproliferative activity with IC50 of 6 M. TP-0903 also induces strong G2/M arrest by potently inhibiting Aurora A and B. In CLL B cells from all the patients with CLL, TP-0903 causes a dose-dependent induction of massive apoptosis by targeting phosphorylated Axl, and overcomes CLL BMSC-mediated protection of CLL B cells from apoptosis.
- 體內研究:
In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. [3] In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.
- 細胞實驗: For cell proliferation assays, 45 μL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate media. The following day, TP-0903 is diluted in serum free growth media to 10x desired concentrations and 5 μL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 μL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an microplate reader
- 參考文獻:
1. Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912. 2. Sinha S, et al. Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors. Clin Cancer Res. 2015, 21(9), 2115-2126.
- 溶解性: soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.938 ml 9.689 ml 19.378 ml 5 mM 0.388 ml 1.938 ml 3.876 ml 10 mM 0.194 ml 0.969 ml 1.938 ml 50 mM 0.039 ml 0.194 ml 0.388 ml
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質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)