性能参数

产品名称

Ilorasertib (ABT-348)

规格

1mg  5mg 10mg 20mg

货号

GOY-Y3716

 含量

>98.00%

CAS

1227939-82-3

别名

N/A

化学名

N/A

分子式

C25H21FN6O2S

分子量

分子量 488.54

溶解度

DMSO : 83.33 mg/mL (170.57 mM);H2O : < 0.1 mg/mL (insoluble)

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

Ilorasertib (ABT-348) is an ATP-competitive multitargeted kinase inhibitor with IC50s for inhibiting binding Aurora B (7 nM), C (1 nM), and A (120 nM), and also inhibits RET tyrosine kinase, PDGFRβ, and Flt1 with IC50s of 7 nM, 3 nM and 32 nM.

Ilorasertib is an ATP-competitive multitargeted kinase inhibitor with IC50 for inhibiting cellular autophosphorylation of Aurora B (13 nM), C (13 nM), and A (189 nM). In addition to targeting Aurora kinases, Ilorasertib is a potent inhibitor of the VEGFR and PDGFR kinase families and, to a lesser extent, the Src family of cytoplasmic tyrosine kinases. Ilorasertib induces a concentration-dependent increase in the extent and number of two NSCLC cell lines exhibiting polyploidy. The potency for inducing this response (EC50 = 5 and 10 nM). Ilorasertib shows antiproliferative activity against BCR-ABL expressing CML cells and cells expressing the gleevec-resistant BCR-ABL T315I mutation (IC50 = 47 and 260 nM)[2].

Ilorasertib (25 mg/kg, s.c.) leads to an inhibition of histone H3 phosphorylation in circulating tumor cells obtained from an engrafted leukemia model. Ilorasertib inhibits the VEGF response with a potency (ED50 = 0.2 mg/kg i.v.) in a uterine edema model. Ilorasertib (20 mg/kg, p.o.) inhibits the growth of established tumors and causes regression of advanced tumors in human xenograft models[2]. Ilorasertib demonstrates significant antitumor efficacy in both solid and hematological xenograft models after intravenous, mini-pump or parenteral once-weekly dosing[3].

2-羟基-3,5-二硝基吡啶  2980-33-8  2-溴-4-苯基乙酰苯  135-73-9

2-正己基噻吩  18794-77-9  3-甲氧基肉桂酸  1533748

4-甲基-3-硝基苯甲醛  31680-07-6  氯化胆碱  67-48-1

4-氯-2-甲基苯甲酸  2045177  茚  95-13-6

氧化钌  32740-79-7  苯甲醛-2-磺酸钠  1008-72-6

六水硫酸镍  10101-97-0  3-氯-2,4,5-三氟苯甲酸  101513-77-3

3-氯酚3-Chlorophenol,98%108-43-025G

2,3,5-**基苯酚2,3,5-Trimethylphenol,99%697-82-525G

2-氯-4-硝基酚2-Chloro-4-nitrophenol,97%619-08-95G

对溴苯酚4-Bromophbenol,99%106-41-225G

混合甲酚Cresol mixed isomers,99%1319-77-325ML

间苯三酚,无水Phloroglucinol,≥99.0%108-73-625G