Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Debio 0932 is an orally active inhibitor of HSP90 (IC50s: 100 and 103 nM for HSP90α and HSP90β, respectively).
产品描述 | Debio 0932 is an orally active inhibitor of HSP90 (IC50s: 100 and 103 nM for HSP90α and HSP90β, respectively). |
靶点活性 | HSP90 β:103 nM, HSP90 α:100 nM |
体外活性 | Debio 0932 also displays inhibitory activities against the proliferation of 40 cancer cell lines (containing 34 solid and 6 hematologic tumor-derived lines) (IC50 ranging from 40 to 900 nM) (mean IC50, 220 nM) [1]. Debio 0932 binds to the tumor HSP90 complex( a mean IC50: 48.8 nM). Debio 0932 (1 μM) promotes degradation of multiple HSP90 client proteins in cancer cell lines. Debio 0932 potently binds to cancer-derived HSP90 complex (IC50: 61.2 nM in H1975 cells and 74.2 nM in H1993 cells, respectively). Debio 0932 (CUDC-305, 1 μM) durably induces oncoprotein degradation in NSCLC cell lines with mutations that can confer resistance to erlotinib [3]. |
体内活性 | Debio 0932 is able to cross the blood-brain barrier. Debio 0932 (30 mg/kg, p.o.) exhibits favorable pharmacokinetic profiles in tumor-bearing nude mice. Debio 0932 (80 mg/kg, p.o.) significantly alleviates psoriasis by day 11 and decreases epidermal thickness in psoriasis xenograft transplantation model [2]. Debio 0932 (160 mg/kg, p.o.) causes degradation of HSP90 client proteins, suppresses tumor growth, and also prolongs survival in various animal models of U87MG glioblastoma. Debio 0932 (160 mg/kg, p.o.) also promotes antitumor activity in the erlotinib-resistant H1975 subcutaneous tumor model. Debio 0932 (40, 80, or 160 mg/kg, p.o.) also dose-dependently inhibits tumor growth in the U87MG s.c. tumor model by every-other-day (q2d) dosing [1]. Debio 0932 (80, 120, and 160 mg/kg, p.o.) displays dose-dependent inhibition of tumor growth in the H1975 subcutaneous tumor model [3]. |
别名 | CUDC-305 |
分子量 | 442.58 |
分子式 | C22H30N6O2S |
CAS No. | 1061318-81-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33 mg/mL (74.56 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2595 mL | 11.2974 mL | 22.5948 mL | 56.487 mL |
5 mM | 0.4519 mL | 2.2595 mL | 4.519 mL | 11.2974 mL | |
10 mM | 0.2259 mL | 1.1297 mL | 2.2595 mL | 5.6487 mL | |
20 mM | 0.113 mL | 0.5649 mL | 1.1297 mL | 2.8243 mL | |
50 mM | 0.0452 mL | 0.2259 mL | 0.4519 mL | 1.1297 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Debio 0932 1061318-81-7 Cytoskeletal Signaling Metabolism HSP CUDC 305 CUDC-305 CUDC305 Inhibitor inhibitor inhibit