AZD6482 Inhibitor CAS No. 1173900-33-8

Cat. No.	Name	Size	Price
KI0449	AZD6482	5 mg	$272
	AZD6482	10 mg	$350
	AZD6482	50 mg	$1300

Chemical Characteristic

Product Name	AZD6482
Synonyms	KIN-193
CAS No.	1173900-33-8
Molecular Weight	408.45
Formula	C₂₂H₂₄N₄O₄
Chemical Name	2-[[(1R)-1-[7-Methyl-2-(4-morpholinyl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid
Smiles	C(=O)(c1c(cccc1)N[C@H](C)c1c2nc(cc(=O)n2cc(c1)C)N1CCOCC1)O
Chemical Structure

Biological activities

KIN-193 is a potent and selective p110β inhibitor. KIN-193 is efficacious specifically in preventing AKT signaling and tumor growth depending on p110β activation or PTEN loss. KIN-193 strongly inhibits p110β's kinase activity. The IC50 is 0.69 nM. KIN-193 inhibits p110α, p110δ, and p110γ isoforms with lower selectivity. KIN-193 prevents p110β with 200-, 20-, and 70-fold selectivity over other isoforms (p110α, p110δ, and p110γ), respectively. KIN-193 also exhibits selectivity of approximately 80-fold over PI3K-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases. 35% of cell lines with PTEN mutations (20 of 57) and 16% of cell lines with wild-type PTEN (58 of 365) are susceptible to KIN-193 with a threshold of EC50 less than 5 μM. KIN-193 significantly prevents tumor growth of both HCC70 and PC3 tumors based on reducing levels of both AKT phosphorylation and Ki67 signal in xenograft tumors of both PTEN-deficient cancer cell lines, HCC70 and PC3.^[1]

References

[1] Ni J,et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012, 2(5): 425-433.

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