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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-SAR405
SAR405

Chemical Structure : SAR405

CAS No.: 1523406-39-4

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SAR405 (SAR-405;SAR 405)

货号: PC-43055Not For Human Use, Lab Use Only.

SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM.

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

生物&药学活性

SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM.
SAR405 displays no activity against class I and II PI3K isoforms (IC50>10 uM), as well as PIKKs, ATM, ATR and DNA-PK, SMG1.
SAR405 affects both late endosome-lysosome compartments and prevents autophagy, shows synergistic antiproliferative activity in renal tumor cell lines combined with mTOR inhibitor everolimus.
SAR405 enhances the antitumor efficacy of cisplatin in mouse xenograft model of HNSCC.

物理化学性质&存储条件

分子量 443.8506
分子式 C19H21ClF3N5O2
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: ≥ 27 mg/mL
Chemical Name/SMILES

4H-Pyrimido[1,2-a]pyrimidin-4-one, 9-[(5-chloro-3-pyridinyl)methyl]-6,7,8,9-tetrahydro-2-[(3R)-3-methyl-4-morpholinyl]-8-(trifluoromethyl)-, (8S)-

参考文献

1. Ronan B, et al. Nat Chem Biol. 2014 Dec;10(12):1013-9.

2. Pasquier B. Autophagy. 2015 Apr 3;11(4):725-6.

3. Valet C, et al. Blood. 2017 Nov 2;130(18):2032-2042.

4. New J, et al. Cancer Res. 2017 Dec 1;77(23):6679-6691.

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