产品名称

英文名称：Pilaralisib (XL147)

同义词

Pilaralisib、934526-89-3、XL-147、SAR245408、SAR-245408、2-Amino-n-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide、2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide

产品性质

CAS编号：934526-89-3

分子式：C25H25ClN6O4S

分子量：541.02

PubChem编号：56599306

英文别名：Pilaralisib|934526-89-3|XL-147|SAR245408|SAR-245408|2-Amino-n-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide|2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide

规格或纯度：≥98%

英文名称：Pilaralisib (XL147)

生化机理：DescriptionIC50 Value39 nM (PI3Kα); 383 nM (PI3Kβ); 36 nM (PI3Kδ); 23 nM(PI3Kγ) [1]XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values in the nanomolar range in biochemical assays.in vitro XL147 binds in an ATP-competitive and reversible manner, yet is highly selective against a panel of >130 human protein kinases. In cellular assays, XL147 antagonizes the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) resulting in inhibition of phosphorylation of several downstream effectors of PI3K including Akt, ribosomal S6 kinase, and ribosomal S6 protein [1].Compared with XL147 alone, the combination exhibited a superior antitumor effect against trastuzumab-resistant tumor xenografts. Furthermore, treatment with XL147 and trastuzumab reduced the cancer stem-cell (CSC) fraction within trastuzumab-resistant cells both in vitro and in vivo [2].

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：25mg、100mg卖完停产，不再备货

产品介绍：Pilaralisib (XL147)是一种选择性的可逆I型PI3K抑制剂，作用于PI3Kα/δ/γ，在无细胞试验中IC50为 39 nM/36 nM/23 nM，对PI3Kβ作用较低。Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ.

ALogP：3.4

IUPAC Name：2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide

INCHI：InChI=1S/C25H25ClN6O4S/c1-25(2,27)24(33)28-15-7-6-8-17(13-15)37(34,35)32-23-22(29-19-9-4-5-10-20(19)30-23)31-21-14-16(36-3)11-12-18(21)26/h4-14H,27H2,1-3H3,(H,28,33)(H,29,31)(H,30,32)

InChi Key：QINPEPAQOBZPOF-UHFFFAOYSA-N

Canonical SMILES：CC(C)(C(=O)NC1=CC(=CC=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=C(C=CC(=C4)OC)Cl)N

Isomeric SMILES：CC(C)(C(=O)NC1=CC(=CC=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=C(C=CC(=C4)OC)Cl)N

PubChem CID：56599306

溶解性：25°C DMSO 3 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL

象形图：

信号词：Danger

危险声明：H302 Harmful if swallowedH372 Causes damage to organs through prolonged or repeated exposure

预防措施声明：P501,P264,P260,P270,P330,P301+P317,P319

产品包装