| Cas No.: | 1252594-99-2 |
| 名称: | |
| 别名: | ETP46321,ETP 46321 |
| SMILES: | CS(=O)(=O)N1CCN(CC1)CC2=CN3C=C(N=C(C3=N2)N4CCOCC4)C5=CN=C(N=C5)N |
| 分子式: | C20H27N9O3S |
| 分子量: | 473.55 |
| 纯度: | |
| 保存条件: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | |
| In Vivo: | |
| In Vitro: | |
| References: | ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R).ETP-46321, has been pro?led and shown to be a potent PI3K a and d inhibitor, highly selective versus mTOR and 288 representative kinases. The compound demonstrated a good pharmacokinetic profile in mice and was selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-Ras G12V oncogenic mutation, showing significant tumor growth inhibition (ca. 51%), and reduction of the tumor metabolic activity as measured by PET techniques. |
| Kinase Assay: | |
| Cell Assay: | |
| Animal Administration: | |
| References: |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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