BAY 80-6946 Inhibitor CAS No. 1032568-63-0

Cat. No.	Name	Size	Price
KI2065	BAY 80-6946	5 mg	$432
	BAY 80-6946	10 mg	$592
	BAY 80-6946	50 mg	$1712

Chemical Characteristic

Product Name	BAY 80-6946
Synonyms	BAY80-6946, BAY806946
CAS No.	1032568-63-0
Molecular Weight	480.2
Formula	C₂₃H₂₈N₈O₄
Chemical Name	2-amino-n-(2,3-dihydro-7-methoxy-8-(3-(4-morpholinyl)propoxy)imidazo(1,2-c)quinazolin-5-yl)-5-pyrimidinecarboxamide
Smiles	c1(ncc(cn1)C(=O)Nc1nc2c(c3=NCCn13)ccc(c2OC)OCCCN1CCOCC1)N
Chemical Structure

Biological activities

BAY 80-6946 is a potent, selective and reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM. BAY 80-6946 potently inhibits the catalytic activity of the class I PI3Kα, β, γ, and δ isoforms with IC50s of 0.5, 3.7, 6.4, and 0.7 nM, respectively. BAY 80-6946 shows significantly weaker activity against mTOR with an IC50 of 45 nM. In KPL4 cells, BAY 80-6946 reduces pAKT levels at both Thr308 and Ser473 with IC50s of 0.4 and 0.6 nM, respectively. BAY 80-6946 potently inhibits tumor cell proliferation in a subset of human cancer cell lines with PIK3CA mutations and/or over-expression of HER2 in vitro. In addition, BAY 80-6946 treatment also induces apoptosis in a subset of tumor cell lines that are resistant to lapatinib and trastuzumab. In vivo, intravenous administration of BAY 80-6946 is highly efficacious in rat and mouse tumor xenograft models. Moreover, BAY 80-6946 administration induces 100% complete tumor regression when dosed as a single agent every second day in rats bearing HER2-amplified and PIK3CA-mutated KPL4 breast tumors.^[1]

Protocols

In vitro: Prior to use, BAY 80-6946 is dissolved in dimethyl sulfoxide (DMSO) with 10 mM trifluoroacetic acid.^[1]

References

[1] Liu N, et al. BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110? and p110? Activities in Tumor Cell Lines and Xenograft Models. Mol Cancer Ther. 2013, 12: 2319-2330.

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