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Chemical Structure : RLY-2608
CAS No.: 2733573-94-7
Catalog No.: 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.
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| 2 mg | $588 | In stock | |
| 5 mg | $898 | In stock | |
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| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 608.91 | |
| Formula | C29H14ClF5N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Varkaris A, et al. Cancer Discov. 2023 Nov 2. doi: 10.1158/2159-8290.CD-23-0944.
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