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首页-小分子抑制剂&激动剂-Others-Other Targets-IACS-010759
IACS-010759

Chemical Structure : IACS-010759

CAS No.: 1570496-34-2

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IACS-010759 (IACS010759, IACS10759)

货号: PC-35205Not For Human Use, Lab Use Only.

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 99.29% (HPLC) Select Batch:

生物&药学活性

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.
IACS-010759 decreases cell viability and increases apoptosis with EC50 values between 1 nM-50 nM across multiple lines.
IACS-010759 robustly inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, reduces aspartate production that leads to impaired nucleotide biosynthesis.
IACS-010759 potently inhibits tumor growth of brain cancer and AML in vivo.

物理化学性质&存储条件

分子量 562.568
分子式 C25H25F3N6O4S
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

5-(5-methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole

参考文献

1. Molina JR, et al. Nat Med. 2018 Jun 11. doi: 10.1038/s41591-018-0052-4.

2. Vangapandu HV, et al. Oncotarget. 2018 May 18;9(38):24980-24991.

3. Lissanu Deribe Y, et al. Nat Med. 2018 Jun 8. doi: 10.1038/s41591-018-0019-5.

4. Jennifer Molina, et al. Abstract 4971: IACS-010759, a novel inhibitor of complex I in Phase I clinical development to target OXPHOS dependent tumors. AACR. DOI: 10.1158/1538-7445.

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