Oncrasin 1 |
| カタログ番号GC14860 |
抗がん剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 75629-57-1
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | 1-[(4-chlorophenyl)methyl]indole-3-carbaldehyde | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C=O | ||
| Formula | C16H12CINO | M.Wt | 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 | Storage | Store at 4°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7074 mL | 18.5371 mL | 37.0741 mL |
| 5 mM | 741.5 μL | 3.7074 mL | 7.4148 mL |
| 10 mM | 370.7 μL | 1.8537 mL | 3.7074 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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