Basic information Safety Supplier Related

AZD8186

Basic information Safety Supplier Related

AZD8186 Basic information

Product Name:
AZD8186
Synonyms:
  • AZD8186;AZD-8186;AZD 8186
  • CS-1576
  • 8-(1-((3,5-difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide
  • AZD-8186;AZD 8186
  • AZD8186
  • AZD 8186, >=98%
  • (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide
  • 8-[(1R)-1-[(3,5-Difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-6-carboxamide
CAS:
1627494-13-6
MF:
C24H25F2N3O4
MW:
457.47
Mol File:
1627494-13-6.mol
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AZD8186 Chemical Properties

Melting point:
226-227°C
Boiling point:
645.2±55.0 °C(Predicted)
Density 
1.351±0.06 g/cm3(Predicted)
storage temp. 
-20°C Freezer
solubility 
DMSO (Slightly), Ethanol (Slightly), Methanol (Slightly)
pka
2.56±0.50(Predicted)
form 
Solid
color 
White to Off-White
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AZD8186 Usage And Synthesis

Uses

AZD 8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.

Biological Activity

the pi3k-akt signaling pathway plays a critical role in cell growth, proliferation, motility, and survival. in human cancer, this pathway is activated by several mechanisms, including somatic mutations, deletions, and amplifications. class i pi3ks are further divided into class ia enzymes (pi3kα, pi3kβ, and pi3kδ) and class ib enzymes (pi3kγ). azd8186 is a potent and selective inhibitor of pi3kβ and pi3kδ.

in vitro

azd8186 gave potent inhibition of p-akt in cells sensitive to pi3kβ inhibition and in cells sensitive to pi3kδ inhibition but not to cells sensitive to pi3kα inhibition. the overall kinase selectivity of azd8186 was evaluated in several panels of recombinant protein and lipid kinase assays. 13 did not show significant activity against a panel of 59 protein kinases tested at 1 μm [1].

in vivo

the antitumor activity of azd8186 was evaluated in the pten deficient pc3 prostate tumor xenograft model in nude mice, either at 100 mg/kg b.i.d. without abt coadministration, or at 60, 30, and 10 mg/mg b.i.d. with abt coadministration. higher inhibition was seen in the 60 and 30 mg/kg groups with abt coadministration than in the 100 mg/kg group without abt coadministration [1].

IC 50

0.003 μm for pi3kβ and 0.017 μm for pi3kδ

AZD8186Supplier

Shanghai Taibao Pharmaceutical Technology Co., Ltd. Gold
Tel
13816752554
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1745533547@qq.com
Kaixin Chemical (Hong Kong) Limited Gold
Tel
010-88886666-01 13112345678
Email
loyson@tcypharm.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
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+86-21-20908456
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sales@BioChemBest.com
Shanghai Hanhong Scientific Co.,Ltd.
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021-54306202 13764082696
Email
info@hanhongsci.com