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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-AZD8835
AZD8835

Chemical Structure : AZD8835

CAS No.: 1620576-64-8

AZD8835 (AZD-8835)

货号: PC-43269Not For Human Use, Lab Use Only.

AZD8835 (AZD-8835) is a potent, selective inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 and 5.7 nM, 15-fold and >100-fold selectivity over PI3Kγ and PI3Kβ.

规格 价格 库存 数量
10 mg ¥1280 In stock
25 mg ¥1980 In stock
50 mg ¥3280 In stock
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD8835 (AZD-8835) is a potent, selective inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 and 5.7 nM, 15-fold and >100-fold selectivity over PI3Kγ and PI3Kβ.
AZD8835 also potently inhibits PI3Kα mutants E545K and H1047R with IC50 of 6 nM.
AZD8835 preferentially inhibits growth in cells with mutant PIK3CA status inhibits AKT phosphorylation with IC50 of 58 nM in PIK3CA mutant human breast ductal carcinoma BT474 cell line.
AZD8835 suppresses tumour growth (93% tumour growth inhibition) in murine H1047R PI3Kα mutated SKOV-3 xenograft tumour model (25mg/kg b.i.d).

物理化学性质&存储条件

分子量 469.54
分子式 C22H31N9O3
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

DMSO: 16 mg/mL

Chemical Name/SMILES

1-Propanone, 1-[4-[5-[5-amino-6-[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]-2-pyrazinyl]-1-ethyl-1H-1,2,4-triazol-3-yl]-1-piperidinyl]-3-hydroxy-

参考文献

1. Barlaam B, et al. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62.

2. Hudson K, et al. Mol Cancer Ther. 2016 May;15(5):877-89.

3. Lynch JT, et al. Oncotarget. 2016 Apr 19;7(16):22128-39.

4. Maynard J, et al. PLoS One. 2017 Aug 14;12(8):e0183048.

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