产品名称

英文名称：CH5132799

同义词

CH5132799、1007207-67-1、CH-5132799、5-(7-(methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine、izorlisib、CH 5132799、CHEMBL1684984、CH5132799 (PA-799)、JCL936W835、PA799、PA-799、5-(7-Methanesulfonyl-2-Morpholin-4-Yl-6,7-Dihy

产品性质

CAS编号：1007207-67-1

分子式：C15H19N7O3S

分子量：377.42

PubChem编号：49784945

英文别名：CH5132799|1007207-67-1|CH-5132799|5-(7-(methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine|izorlisib|CH 5132799|CHEMBL1684984|CH5132799 (PA-799)|JCL936W835|PA799|PA-799|5-(7-Methanesulfonyl-2-Morpholin-4-Yl-6,7-Dihy

规格或纯度：≥97%

英文名称：CH5132799

生化机理：CH5132799 selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 0.014, 0.12, 05.0, and 0.36 μM, respectively. CH5132799 shows less inhibition of class II PI3Ks, class III PI3ks, and mTOR. CH5132799 suppresses phosphorylation of treated breast cancer KPL-4 cells, as well as Akt and its direct substrates, PRAS40 and FoxO1/3a. Down stream factors, including S6K, S6 and 4E-BP1, are effectively suppressed. Cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH5132799. In human tumor cell lines with PI3K pathway activation by mutation, CH5132799 shows potent antiproliferative activity [HCT116(CRC) IC50 = 0.20 lM, KPL-4(BC)13 IC50 = 0.032 lM, T-47D(BC) IC50 = 0.056 lM, SK-OV-3(Ovarian) IC50 = 0.12 lM].

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：CH5132799是I型PI3K选择性抑制剂，对PI3Kα，PI3Kβ，PI3Kδ和PI3Kγ的IC50分别为0.014，0.12，0.50和0.36 uM，对II和III型PI3k以及mTOR的抑制性较低。A PI3K and FRAP inhibitorCH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines.A PI3K and FRAP inhibitor

ALogP：-0.6

PubChem SID：488201430

PubChem SID url：https//pubchem.ncbi.nlm.nih.gov/substance/488201430

IUPAC Name：5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine

INCHI：InChI=1S/C15H19N7O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21/h8-9H,2-7H2,1H3,(H2,16,17,18)

InChi Key：JEGHXKRHKHPBJD-UHFFFAOYSA-N

Canonical SMILES：CS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N

Isomeric SMILES：CS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N

PubChem CID：49784945

CAS Registry No.：1007207-67-1

ChEMBL Ligand：CHEMBL1684984

RCSB PDB Ligand：MMD

溶解性：DMSO 12 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

产品包装