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首页-小分子抑制剂&激动剂-Apoptosis-MDM2-p53-AMG 232
AMG 232

Chemical Structure : AMG 232

CAS No.: 1352066-68-2

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AMG 232 (Navtemadlin;AMG232;AMG-232)

货号: PC-42959Not For Human Use, Lab Use Only.

Navtemadlin (AMG-232) is a potent, selective, orally bioavailable MDM2-p53 inhibitor with Kd of 0.045 nM, inhibits SJSA-1 cell proliferation with IC50 of 9.1 nM.

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5 mg ￥1380 In stock
10 mg ￥2280 In stock
25 mg ￥3880 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

Navtemadlin (AMG-232) is a potent, selective, orally bioavailable MDM2-p53 inhibitor with Kd of 0.045 nM, inhibits SJSA-1 cell proliferation with IC50 of 9.1 nM.
Navtemadlin (AMG-232) robustly induces p53 activity, leading to cell-cycle arrest and inhibition of tumor cell proliferation.
Navtemadlin (AMG-232) significantly inhibits tumor growth in SJSA-1 osteosarcoma xenograft model with ED50 of 9.1 mg/kg, also showsignificantly superior antitumor efficacy chombined with chemotherapies in vivo, enhances radiosensitivity via inhibition of damage repair signaling.

物理化学性质&存储条件

分子量 568.5522
分子式 C28H35Cl2NO5S
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

3-Piperidineacetic acid, 5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-1-[(1S)-2-methyl-1-[[(1-methylethyl)sulfonyl]methyl]propyl]-2-oxo-, (3R,5R,6S)-

参考文献

1. Sun D, et al. J Med Chem. 2014 Feb 27;57(4):1454-72.

2. Canon J, et al. Mol Cancer Ther. 2015 Mar;14(3):649-58.

3. Werner LR, et al. Mol Cancer Ther. 2015 Sep;14(9):1994-2003.

4. Prabakaran PJ, et al. Clin Cancer Res. 2017 Oct 15;23(20):6044-6053.

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