BAY80-6946

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Cat No.

CEI-0834

Description

BAY 80-6946 is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM. Phase 1.

CAS_No

1032568-63-0

Molecular Weight

480.52

Storage

2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.

Targets

PI3Kα, PI3Kβ

IC50

0.469 nM; 3.72 nM

Molecular Formula

C23H28N8O4

Chemical Name

5-Pyrimidinecarboxamide, 2-amino-N-[2,3-dihydro-7-methoxy-8-[3-(4-morpholinyl)propoxy]imidazo[1,2-c]quinazolin-5-yl]-

Solubility

DMSO 0.002 mg/mL; Water 0.002 mg/mL; Ethanol 0.01 mg/mL

In vitro

BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. BAY 86-9766 inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines.

In vivo

BAY 80-6946 is generally well tolerated through the MTD (maximum tolerated dose) of 0.8 mg/kg. PK (pharmacokinetics) results support weekly dosing. Grade 2/3 hyperglycemia in the first 24 hrs after receiving a dose is common at the MTD. PK, clinical SD and FDG-PET data are consistent with effective exposure and PI3K pathway inhibition.

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Project Description:

For research and industrial use only, not for personal medicinal use.

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