Oncrasin 1
(Synonyms: 1-(4-氯苄基)-1H-吲哚-3-甲醛) 目录号 : GC14860
An anticancer agent
Cas No.:75629-57-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Oncrasin 1 is a small molecule antitumor agent with IC50 value of 4.81 μM [1].
The activated mutations of Ras genes (K-Ras, N-Ras and H-Ras) play important roles in tumorigenesis and maintenance of malignant phenotypes. The mutations make Ras constitutively be in the activated state with GTP-bound. Among the three Ras genes, the mutations of K-Ras are the most frequently found in tumors and are associated with resistance to radio therapy, chemotherapy and poor prognosis. Thus, mutant K-Ras is important target for antitumor treatment. Oncrasin 1 is a small-molecule compound that found by a synthetic lethality screening. It effectively killed tumor cells with K-Ras mutation but not normal isogenic cells through inducing cell apoptosis. Besides that, Oncrasin 1 caused abnormal aggregation of PKCι of those sensitive cells [1].
In a sulforhodamine B (SRB) assay, treatment of Oncrasin 1 at final concentration of 5 μg/ml killed more than 50% of cells. Oncrasin 1 was highly selective against K-Ras mutation, it showed dose-dependent cytotoxicity in T29Kt1 (K-Ras mutant) cells with IC50 value of 4.81 μM. For T29Ht1 (H-Ras mutant) cells and T29 (wild-type Ras) cells, Oncrasin 1 showed no cytotoxicity even at concentration of 33 μM. For the other K-Ras-mutant tumor cells such as A549, H2122 and H460, Oncrasin 1 all showed cytotoxicity with IC50 value of ≤ 3 μM. It was found that induction of apoptosis was a major mechanism of Oncrasin 1 treatment [1].
In mice injected with H460 cells, administration of Oncrasin 1 at dose of 100 mg/kg resulted in significant tumor growth suppression by 75.4%. In addition, the survival time was prolonged by the Oncrasin 1 treatment [1].
Reference:
[1] Guo W, Wu S, Liu J, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer research, 2008, 68(18): 7403-7408.
| Cas No. | 75629-57-1 | SDF | |
| 别名 | 1-(4-氯苄基)-1H-吲哚-3-甲醛 | ||
| 化学名 | 1-[(4-chlorophenyl)methyl]indole-3-carbaldehyde | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C=O | ||
| 分子式 | C16H12CINO | 分子量 | 269.73 |
| 溶解度 | DMF: 10 mg/mL,DMSO: 17 mg/mL,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL,Ethanol: 5 mg/mL | 储存条件 | Store at 4°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7074 mL | 18.5371 mL | 37.0741 mL |
| 5 mM | 0.7415 mL | 3.7074 mL | 7.4148 mL |
| 10 mM | 0.3707 mL | 1.8537 mL | 3.7074 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。