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Oncrasin-1

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Chemical Structure| 75629-57-1 同义名 : -
CAS号 : 75629-57-1
货号 : A746103
分子式 : C16H12ClNO
纯度 : 99%+
分子量 : 269.726
MDL号 : MFCD01051808
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(389.28 mM),配合低频超声助溶,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 The oncogenic gene K-Ras mutations are frequently found in various cancers and are associated with resistance to treatment or poor prognosis. Oncrasin-1 is a potent and effective anticancer inhibitor against various lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 induced dose-dependent cytotoxicity in T29Kt1 cells with an IC50 of 4.81 μM. Oncrasin-1 effectively killed K-Ras–mutant H460, H2122, H2887, and A549 cells with an IC50 of ≤3 μM. Oncrasin-1 (10 μM) effectively induced cell killing in T29Kt1 and H460 cells. Additionally, treatment of H460 cells with 1 μM oncrasin-1 effectively activated caspases 3 and 8. Oncrasin-1 (100 mg/kg/injection daily for 10 days) suppressed tumor growth by 75.4% in mice. Treatment with oncrasin-1 also prolonged survival: the mean survival times for mice treated with solvent and oncrasin-1 were 24 and 32, respectively, demonstrating that Oncrasin-1 might be useful for the treatment of cancers with K-Ras mutations[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.54mL

3.71mL

1.85mL

37.07mL

7.41mL

3.71mL

参考文献

[1]Guo W, Wu S, et al. Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl] -1H-indole-3-carboxaldehyde (oncrasin-1). Mol Cancer Ther. 2009 Feb;8(2):441-8.

[2]Guo W, Wu S, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer Res. 2008 Sep 15;68(18):7403-8.

[3]Guo W, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer Res. 2008 Sep 15;68(18):7403-8.