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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-ON123300
ON123300

Chemical Structure : ON123300

CAS No.: 1357470-29-1

ON123300 (ON-123300, Narazaciclib)

货号: PC-43121Not For Human Use, Lab Use Only.

Narazaciclib (ON123300) is a potent, multi-targeted kinase inhibitor with IC50 of 5, 3.9, 26, 26, 9.2 and 11 nM for ARK5, CDK4, PDGFRβ, FGFR1, RET and FYN, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Narazaciclib (ON123300) is a potent, multi-targeted kinase inhibitor with IC50 of 5, 3.9, 26, 26, 9.2 and 11 nM for ARK5, CDK4, PDGFRβ, FGFR1, RET and FYN, respectively.
Narazaciclib (ON123300) inhibits U87 glioma cell proliferation with IC50 3.4 uM, and reduces phosphorylation of Akt, yet it also unexpectedly induces Erk activation and prevents phosphorylation of C-Raf S259.
Narazaciclib (ON123300) suppresses phosphorylation of Akt as well as activation of Erk in brain tumors in vivo.
Narazaciclib (ON123300) also exhibits potent activity against mantle cell lymphomas both in vitro and in vivo, triggers apoptosis and inhibition of the Rb and PI3K/AKT pathways.

物理化学性质&存储条件

分子量 429.5175
分子式 C24H27N7O
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

Pyrido[2,3-d]pyrimidine-6-carbonitrile, 8-cyclopentyl-7,8-dihydro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-7-oxo-

参考文献

1. Zhang X, et al. Mol Cancer Ther. 2014 May;13(5):1105-16.

2. Divakar SK, et al. Leukemia. 2016 Jan;30(1):86-93.

3. Perumal D, et al. Cancer Res. 2016 Mar 1;76(5):1225-36.

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