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Chemical Structure : ETP-46321
CAS No.: 1252594-99-2
Catalog No.: PC-42989Not For Human Use, Lab Use Only.
ETP-46321 is a potent, selective, orally bioavailable dual PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM, weakly inhibits p110β and p110γ with IC50 of 170 and 179 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $218 | In stock | |
| 10 mg | $368 | In stock | |
| 25 mg | $528 | In stock | |
| 100 mg | Get quote |
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ETP-46321 is a potent, selective, orally bioavailable dual PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM, weakly inhibits p110β and p110γ with IC50 of 170 and 179 nM.
ETP-46321 shows highly selectivity versus mTOR and 288 representative kinases, also potently inhibits mutants PI3K α E542K, E545K, and H1047R with IC50 of ~2 nM.
ETP-46321 inhibits phosphorylation of AKT Ser473 in the U2OS cell line with IC50 of 8.3 nM.
ETP-46321 shows significant tumor growth inhibition and reduction of the tumor metabolic activity in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation.
| M.Wt | 473.5519 | |
| Formula | C20H27N9O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 33 mg/mL |
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| Chemical Name/SMILES |
2-Pyrimidinamine, 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]- |
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1. Martínez González S, et al. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6.
2. Granda TG, et al. Invest New Drugs. 2013 Feb;31(1):66-76.
3. Aragoneses-Fenoll L, et al. Biochem Pharmacol. 2016 Apr 15;106:56-69.
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