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CAS No.: 1118460-77-7

UCPH-101 Catalog No. CSN21219

Synonyms: UCPH-101

UCPH 101 selectively but not competitively inhibit excitatory amino acid transporter 1 (EAAT1) with IC50 of 660 nM. It exhibits relatively weak inhibition of other subtypes.

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述ON 123300 is multikinase inhibitor with 3.87, 9.82, 4.95, 26, 26 and 144nM for Cdk4/cyclin D1, CDK6/cyclinD1, ARK5, FGFR1, PDGFRβ and PI3K-δ, respectively. ON 123300 exhibited potent activity against mantle cell lymphomas Z138C and GRANTA 519 with GI50 values of 25nM and 35nM, respectively, as well as inhibited the proliferation of cell lines of different tumor types with GI50 values ranging in 0.1-0.6μM. As a dual inhibitor of both Cdk4/6 and PI3K-δ, ON123300 inhibited phosphorylation of both Rb family proteins and proteins associated with the PI3K/AKT pathway, at concentration of 2.5-10μM post 24h, with apoptosis observed. Treatment of ibrutinib-sensitive and -resistant patient-derived MCLs with ON123300 also triggered apoptosis and inhibition of the Rb and PI3K/AKT pathways. Administration of ON 123300 at dose of 100mg/kg, i.p., daily for 2 weeks significantly inhibited tumor growth in a nude mouse model of Z138C MCL.
动物研究
剂量
Rat: 10 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Rat: 10 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Divakar SK, Ramana Reddy MV, et al. Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas. Leukemia. 2016 Jan;30(1):86-93.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3670 mL
- 11.8350 mL
- 23.6700 mL
- 5 mM
- 0.4734 mL
- 2.3670 mL
- 4.7340 mL
- 10 mM
- 0.2367 mL
- 1.1835 mL
- 2.3670 mL

技术信息

CAS号

1118460-77-7

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H22N2O3

运输

蓝冰

分子量

422.48

别名

UCPH-101

溶解度

DMSO	50.0 mg/mL (118.4 mM)

动物实验配方

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