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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Aurora Kinase-Ilorasertib
Ilorasertib

Chemical Structure : Ilorasertib

CAS No.: 1227939-82-3

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Ilorasertib (ABT-348, ABT348)

货号: PC-21147Not For Human Use, Lab Use Only.

Ilorasertib (ABT-348) is a potent inhibitor of Aurora kinases as well as the VEGF and PDGF families of receptor tyrosine kinases (Aur B IC50=2 nM, PDGFRβ IC50=3 nM).

规格 价格 库存 数量
5 mg ￥2280 In stock
10 mg ￥3780 In stock
25 mg ￥5880 In stock
100 mg Get quote
1 g Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ilorasertib (ABT-348) is a potent inhibitor of Aurora kinases as well as the VEGF and PDGF families of receptor tyrosine kinases (Aur B IC50=2 nM, PDGFRβ IC50=3 nM).
Ilorasertib (ABT-348) inhibits phosphorylation of histone H3, induces of polyploidy, and inhibits proliferation of a variety of leukemia, lymphoma, and solid tumor cell lines (IC(50) = 0.3-21 nM).
Ilorasertib (ABT-348) shows potent binding activity (K(i) < 30 nM) against VEGFR/PDGFR families and the Src family of cytoplasmic tyrosine kinases.
Ilorasertib (ABT-348) inhibits VEGFR/PDGFR autophosphorylation in cells and inhibition of VEGF-stimulated endothelial cell proliferation (IC(50) ≤ 0.3 nM).
Ilorasertib (ABT-348) exhibits antiproliferative activity against BCR-ABL chronic myeloid leukemia cells and cells expressing the gleevec-resistant BCR-ABL T315I mutation.
Ilorasertib (ABT-348) demonstrates significant antitumor efficacy in representative solid tumor [HT1080 and pancreatic carcinoma (MiaPaCa), tumor stasis] and hematological malignancy (RS4;11, regression) xenografts.

物理化学性质&存储条件

分子量 488.54
分子式 C25H21FN6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-[4-[4-Amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl]phenyl]-N′-(3-fluorophenyl)urea

参考文献

1. Glaser KB, et al. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.

2. Curtin ML, et al. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5.

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