产品名称

英文名称：AZD1152

同义词

2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate 、 AZD1152 (Barasertib) 、 AC-35703 、 CHEBI167636 、 CS-D0326 、 AKOS040741193 、 barasertibum 、 CS-W000582 、 FT-0736007 、 2-(、巴拉塞替

产品性质

CAS编号：722543-31-9

分子式：C26H31FN7O6P

分子量：587.54

PubChem编号：11497983

别名：巴拉塞替

英文别名：2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate | AZD1152 (Barasertib) | AC-35703 | CHEBI167636 | CS-D0326 | AKOS040741193 | barasertibum | CS-W000582 | FT-0736007 | 2-(

规格或纯度：98%

英文名称：AZD1152

生化机理：AZD1152 (barasertib) is a pro-drμg that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML). The MTDs （the maximum-tolerated dose ） were 150 mg as a 48-h continuous infusion and 220 mg administered as two 2-h infusions (110 mg/day, days 1, 2, 15 and 16), with neutropenia the dose-limiting toxicity (DLT) of each schedule. Common Terminology Criteria of Adverse Events The pharmacokinetic (PK), metabolic and excretion profiles of barasertib and barasertib-hQPA were characterized in this open-label Phase I study. Pgp and BCRP positive primary samples were less sensitive to barasertib-hQPA induced pHH3 inhibition (p = <0.001) than samples without these transporters. IC50inhibition of pHH3 by barasertib-hQPA was achieved in 94.6% of these samples after 1 hour drμg treatment, in contrast to the resistance of the cell lines. Common Terminology Criteria of Adverse Events (CTCAE) grade?≥?3 neutropenia (with or without fever) occurred in 34 % of patients overall. Barasertib-hQPA was extensively distributed to tissues, with a slow rate of total clearance (CL = 31.4 L/h). Overall, 72-82 % of radioactivity was recovered, with approximately double the amount recovered in feces (mean = 51 %) compared with urine (mean = 27 %).

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：Barasertib (AZD1152) 是 Barasertib-hQPA 的前体药物，是高度选择性的 Aurora B 抑制剂，IC50 值为 0.37 nM。Barasertib (AZD1152) 可引起癌细胞生长阻滞和凋亡。

ALogP：-0.4

IUPAC Name：2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate

INCHI：InChI=1S/C26H31FN7O6P/c1-2-34(10-12-40-41(36,37)38)9-4-11-39-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(35)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17H,2,4,9-12,15H2,1H3,(H,30,35)(H2,36,37,38)(H2,28,29,31,32,33)

InChi Key：GBJVVSCPOBPEIT-UHFFFAOYSA-N

Canonical SMILES：CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCOP(=O)(O)O

Isomeric SMILES：CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCOP(=O)(O)O

PubChem CID：11497983

CAS Registry No.：722543-31-9

ChEMBL Ligand：CHEMBL415049

溶解性：DMSO > 80 mg/ml Water

产品包装