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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-Debio 0932
Debio 0932

Chemical Structure : Debio 0932

CAS No.: 1061318-81-7

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Debio 0932 (CUDC-305, RGRN-305)

货号: PC-49868Not For Human Use, Lab Use Only.

Debio 0932 (CUDC-305, RGRN-305) is a highly potent, oral and BBB-penetrant HSP90 inhibitor, shows high affinity for HSP90alpha/beta and HSP90 complex derived from cancer cells with IC50 of 100 nM and 48.8 nM, respectively.

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10 mg ￥1880 In stock
25 mg ￥2780 In stock
50 mg ￥4780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Debio 0932 (CUDC-305, RGRN-305) is a highly potent, oral and BBB-penetrant HSP90 inhibitor, shows high affinity for HSP90alpha/beta and HSP90 complex derived from cancer cells with IC50 of 100 nM and 48.8 nM, respectively.
Debio 0932 (CUDC-305) displays potent antiproliferative activity against a broad range of cancer cell lines with mean IC50 of 220 nM.
Debio 0932 (CUDC-305) exhibits dose-dependent antitumor activity in an s.c. xenograft model of U87MG glioblastoma and significantly prolongs animal survival in U87MG orthotopic model.
Debio 0932 (CUDC-305) also displays potent antitumor activity in animal models of erlotinib-resistant non-small cell lung cancer and induces tumor regression in animal models of MDA-MB-468 breast cancer and MV4-11 acute myelogenous leukemia.
Debio 0932 (CUDC-305) binds strongly to HSP90 extracted from erlotinib-resistant NSCLC cells (IC50=70 nM).
Debio 0932 (CUDC-305) potently inhibits tumor growth in subcutaneous xenograft models of H1975 and A549, which harbor EGFR T790M mutation or K-ras mutations conferring acquired and primary erlotinib resistance, respectively.

物理化学性质&存储条件

分子量 442.58
分子式 C22H30N6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((6-(dimethylamino)benzo[d][1,3]dioxol-5-yl)thio)-1-(2-(neopentylamino)ethyl)-1H-imidazo[4,5-c]pyridin-4-amine

参考文献

1. Bao R, et al. Clin Cancer Res. 2009 Jun 15;15(12):4046-57.

2. Bao R, et al. Mol Cancer Ther. 2009 Dec;8(12):3296-306.

3. Isambert N, et al. Ann Oncol. 2015 May;26(5):1005-1011.

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