SAR-260301
Cat. No.:YN420226
产品名称: | SAR-260301 |
CAS No.: | 1260612-13-2 |
Chemical Name: | 2-[2-[(2S)-2,3-dihydro-2-methyl-1H-indol-1-yl]-2-oxoethyl]-6-(4-morpholinyl)-4(3H)-pyrimidinone |
Synonyms: | SAR-260301;SAR 260301 |
分子量: | 354.40 |
分子式: | C₁₉H₂₂N₄O₃ |
SMILES: | O=C1N=C(CC(N2[C@@H](C)CC3=C2C=CC=C3)=O)NC(N4CCOCC4)=C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | SAR-260301 是一种有效的,具有口服活性的选择性PI3Kβ抑制剂,IC50为 23 nM。 |
IC50和靶点: | [{name:"PI3Kβ:23 nM (IC50)"},{name: "PI3Kδ:468 nM (IC50)"},{name: "PI3Kα:1539 nM (IC50)"},{name: "PI3Kγ:10000 nM (IC50)"},{name: "Vps34:183 nM (IC50)"},{name: "PI3KC2γ:3812 nM (IC50)"},{name: "pAkt:49 nM (IC50)"},{name: "DNA-PK:2000 nM (IC50)"}] |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Certal, V., Carry, J.C., Halley, F., et al.Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancersJ. Med. Chem.57(3),903-920(2014)
Bonnevaux, H., Lemaitre, O., Vincent, L., et al.Concomitant inhibition of PI3Kβ and BRAF or MEK in PTEN-deficient/BRAF-mutant melanoma treatment: Preclinical assessment of SAR260301 oral PI3Kβ-selective inhibitorMol. Cancer Ther.15(7),1460-1471(2016)