PIK-75 Hydrochloride

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Chemical Information

Product name：PIK-75 Hydrochloride	Purity：98% min
CAS NO：372196-77-5	Solubility：DMSO : ≥ 30 mg/mL (61.38 mM)
Molecular Formula：C₁₆H₁₅BrClN₅O₄S	Package：Package according to customer requirements
Molecular Weight：488.743	Storage：Store at -20℃

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Remarks

PIK-75 was developed as part of a PI 3-kinase drug discovery program. PIK75 attenuates insulin stimulation of Akt/PKB in a range of cell types at 100 nM. The compound has been reported to block growth of a range of cell lines with an IC50 value in the region of 50 nM. In vivo studies have shown that PIK-75, administered at 50 mg/kg, inhibited the growth of HeLa cell xenografts in mice models.

PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.

Related Products:

Alpelisib; Gedatolisib; AS-604850; CAY10505; AS-605240; Apitolisib; PIK-93; YM201636; ZSTK474; PI-103; PD98059; GNE-493; MTX-211; AKTIV; Duvelisib; TGX-221; LY294002

References

[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[2]. Zheng Z, et al. Isoform-selective inhibition of phosphoinositide 3-kinase: identification of a new region of nonconserved amino acids critical for p110α inhibition. Mol Pharmacol. 2011 Oct;80(4):657-64.