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UCPH-101

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Chemical Structure| 1118460-77-7 同义名 : -
CAS号 : 1118460-77-7
货号 : A673822
分子式 : C27H22N2O3
纯度 : 98%+
分子量 : 422.475
MDL号 : MFCD12913298
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(118.35 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.84mL

2.37mL

1.18mL

23.67mL

4.73mL

2.37mL
参考文献

[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.