RLY-2608 | PI3Kα mutants inhibitor | Probechem Biochemicals

Chemical Structure : RLY-2608

CAS No.: 2733573-94-7

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RLY-2608 (RLY2608, RLY 2608)

货号: PC-21298Not For Human Use, Lab Use Only.

RLY-2608 (RLY2608) is a first-in-class, allosteric, mutant-selective inhibitor of PI3Kα with IC50 of 4 nM (PI3Kα H1047R), 12-fold selective over PI3Kα WT.

规格	价格	库存
2 mg	￥5880	In stock
5 mg	￥8980	In stock
10 mg		Get quote
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

RLY-2608 (RLY2608) is a first-in-class, allosteric, mutant-selective inhibitor of PI3Kα with IC50 of 4 nM (PI3Kα H1047R), 12-fold selective over PI3Kα WT.
RLY-2608 is active in cells against tail and helical domain PIK3CA mutations.
RLY-2608 is highly selective over PI3K isoforms and does not detectibly inhibit other kinases.
RLY-2608 (100 mg/kg) inhibits tumors in animal models with reduced impact on insulin levels.
RLY-2608 can maximally inhibit tumors driven by mutations impacting the regulation of PI3Kα while mitigating the hyperglycemia adverse effect that result from inhibiting WT protein.

物理化学性质&存储条件

分子量	608.91
分子式	C29H14ClF5N6O2
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	(R)-N-(3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxoisoindolin-4-yl)-3-fluoro-5-(trifluoromethyl)benzamide

参考文献

1. Varkaris A, et al. Cancer Discov. 2023 Nov 2. doi: 10.1158/2159-8290.CD-23-0944.

RLY-2608 (RLY2608, RLY 2608)

生物&药学活性

物理化学性质&存储条件

参考文献

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RLY-2608 (RLY2608, RLY 2608)

生物&药学活性

物理化学性质&存储条件

参考文献

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