[CAS NO. 1627494-13-6] AZD8186
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PRODUCTS SPECIFICATIONS [1627494-13-6]
Distributor
Catalog
SLK-S7694
Brand
Selleck
CAS
1627494-13-6
DESCRIPTION [1627494-13-6]
Overview
| MDL | MFCD27987908 |
|---|---|
| Molecular Weight | 457.47 |
| Molecular Formula | C24H25F2N3O4 |
| SMILES | O=C(C1=CC(C(C=C(N2CCOCC2)O3)=O)=C3C([C@H](NC4=CC(F)=CC(F)=C4)C)=C1)N(C)C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1859 mL | 10.9297 mL | 21.8594 mL |
| 5 mM | 0.4372 mL | 2.1859 mL | 4.3719 mL |
| 10 mM | 0.2186 mL | 1.0930 mL | 2.1859 mL |
| 50 mM | 0.0437 mL | 0.2186 mL | 0.4372 mL |
Description
AZD8186 is a potent and selective inhibitor of with IC50 of 4 nM and 12 nM, respectively. Phase 1.
In vitro
AZD8186 potently inhibits p-Akt in MDA-MB-468 cells sensitive to PI3Kβ inhibition and Jeko B cells sensitive to PI3Kδ inhibition with IC50 of 3 nM and 4 nM, respectively. AZD8186 shows preferred growth inhibition activity in most PTEN deficient cell lines with GI50 of <1 μM.
In vivo
In nude mice bearing PTEN-deficient PC3 prostate tumor xenografts, AZD8186 (100 mg/kg, p.o.) strongly inhibits Akt phosphorylation levels, and causes significant tumor growth inhibition. When used in combination with ABT, AZD8186 (60 mg/kg, p.o.) results in complete inhibition of tumor growth. In the mouse PTEN-null TNBC models HCC70 and MDA-MB-468, and the prostate models HID28, AZD8186 (50 mg/kg, p.o.) also inhibits the growth of tumors. Combination therapy using AZD8186 with androgen deprivation results in long-lasting tumor regression, which persisted after treatment cessation.
References
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