产品名称

英文名称：XL147

同义词

956958-53-5、XL147、PI3K inhibitor X、N-[3-(2,1,3-benzothiadiazol-5-ylamino)quinoxalin-2-yl]-4-methylbenzenesulfonamide、XL147-II、N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide、N-(3-(benzo[c][1,2,5]thiadiazol-5-ylamino)quino、XL 147、N-[3-(2,1,3-苯并噻唑-5-基氨基)喹恶啉-2-基]-4-甲苯磺酰胺

产品性质

CAS编号：956958-53-5

分子式：C21H16N6O2S2

分子量：448.52

PubChem编号：1893730

别名：XL 147|N-[3-(2,1,3-苯并噻唑-5-基氨基)喹恶啉-2-基]-4-甲苯磺酰胺

英文别名：956958-53-5|XL147|PI3K inhibitor X|N-[3-(2,1,3-benzothiadiazol-5-ylamino)quinoxalin-2-yl]-4-methylbenzenesulfonamide|XL147-II|N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide|N-(3-(benzo[c][1,2,5]thiadiazol-5-ylamino)quino

规格或纯度：≥98%

英文名称：XL147

生化机理：XL-147 derivative 2 is an ATP-competitive inhibitor of class I PI3K isoforms. XL-147 derivative 2 abrogates Akt and S6 phosphorylation in HER2+ cells and also induces the expression and phosphorylation of HER3 and other RTKs. Treatment with the anti-HER2 agents trastuzumab or lapatinib sensitizes HER2+ breast cancer cells to XL-147 derivative 2 in vitro. Treatment with XL-147 derivative 2 inhibits the monolayer growth of all tested cell lines, including BT474, HCC1937 et al. in a dose-dependent manner. XL-147 derivative 2 induces cell death at a concentration of 20 μM by inducing a reduction in cyclin D1 and pRB and increasing in levels of the CDK inhibitor p27KIPI. In HER2-overexpressing cells, inhibition of PI3K is followed by up-regulation of expression and phosphorylation of multiple receptor tyrosine kinases, including HER3.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：XL147是一种选择性的，可逆的I型PI3K抑制剂，对PI3Kα/δ/γ有抑制作用，IC50分别为39 nM/36 nM/23 nM，对PI3Kβ作用效果稍弱。An ATP-competetive class I PI3K inhibitor.XL147 is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM, less potent to PI3Kβ.An ATP-competetive class I PI3K inhibitor.

IUPAC Name：N-[3-(2,1,3-benzothiadiazol-5-ylamino)quinoxalin-2-yl]-4-methylbenzenesulfonamide

INCHI：InChI=1S/C21H16N6O2S2/c1-13-6-9-15(10-7-13)31(28,29)27-21-20(23-16-4-2-3-5-17(16)24-21)22-14-8-11-18-19(12-14)26-30-25-18/h2-12H,1H3,(H,22,23)(H,24,27)

InChi Key：MQMKRQLTIWPEDM-UHFFFAOYSA-N

Canonical SMILES：CC1=CC=C(C=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=CC5=NSN=C5C=C4

Isomeric SMILES：CC1=CC=C(C=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=CC5=NSN=C5C=C4

PubChem CID：1893730

ChEBI：CHEBI71957

CAS Registry No.：956958-53-5

ChEMBL Ligand：CHEMBL3218575

Reactome Reaction：R-HSA-2400009

Reactome Drug：R-ALL-2399886

溶解性：≥22.45 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH

象形图：

信号词：Warning

危险声明：H302 Harmful if swallowed

预防措施声明：P501,P264,P270,P330,P301+P317

产品包装