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快速发货 顺丰冷链运输,1-2 天到达
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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. |
Dose | Rat: 10 mg/kg[2] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.83mL 2.37mL 1.18mL |
23.67mL 4.73mL 2.37mL |
CAS号 | 1118460-77-7 |
分子式 | C27H22N2O3 |
分子量 | 422.48 |
SMILES Code | N#CC1=C(N)OC(CC(C2=C3C=CC=CC3=CC=C2)CC4=O)=C4C1C5=CC=C(OC)C=C5 |
MDL No. | MFCD12913298 |
别名 | |
运输 | 蓝冰 |
InChI Key | YBMGNDPBARCLFT-UHFFFAOYSA-N |
Pubchem ID | 25223366 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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