 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1627494-13-6 |
| Molecular formula(MF) | C24H25F2N3O4 |
| Molecular Weight(MW): | 457.47 |
| Alias |
| In vitro | DMSO | 91 mg/mL warmed (198.92 mM) |
|---|---|---|
| Ethanol | 35 mg/mL warmed (76.5 mM) | |
| Water | <1 mg/mL | |
| In vivo | 10% DMSO + 60% TEG+ 30% WFI | 16mg/mL |
| Description | AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1. | |||||||||||
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| Targets |
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| 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. [1] AZD8186 shows preferred growth inhibition activity in most PTEN deficient cell lines with GI50 of <1 μM. [2] |
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| 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. [1] 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. [2] Combination therapy using AZD8186 with androgen deprivation results in long-lasting tumor regression, which persisted after treatment cessation. [3] |