Oncrasin-1
Based on 1 Customer Validation
Oncrasin-1 is an RNA polymerase inhibitor. Oncrasin-1 suppresses the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells. Oncrasin-1 effectively kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 leads to coaggregation of PKCι and splicing factors into megaspliceosomes. Oncrasin-1 induces malfunction in the RNA processing machinery. Oncrasin-1 is an anti-cancer agent and can therefore be studied in research for lung cancer.
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- Purity: 98.16%
- CAS No.: 75629-57-1
- 화학식: C16H12ClNO
- 분자량:269.73
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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RNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
≤3 μM
Compound: 5
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Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
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[PMID: 23566315] |
| A549 | IC50 |
2.48 μM
Compound: 4, Oncrasin-1
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Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
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[PMID: 25874341] |
| HT-29 | IC50 |
1.71 μM
Compound: 4, Oncrasin-1
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Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
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[PMID: 25874341] |
| MDA-MB-231 | IC50 |
26.1 μM
Compound: 4, Oncrasin-1
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Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 25874341] |
| NCI-H2122 | IC50 |
≤3 μM
Compound: 5
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Cytotoxicity against human NCI-H2122 cells by SRB assay
Cytotoxicity against human NCI-H2122 cells by SRB assay
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[PMID: 23566315] |
| NCI-H460 | IC50 |
0.25 μM
Compound: oncrasin-1
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Cytotoxicity against human H460 cells assessed as cell viability after 3 days by sulforhodamine B assay
Cytotoxicity against human H460 cells assessed as cell viability after 3 days by sulforhodamine B assay
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[PMID: 21443218] |
| NCI-H460 | IC50 |
≤3 μM
Compound: 5
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Cytotoxicity against human H460 cells by SRB assay
Cytotoxicity against human H460 cells by SRB assay
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[PMID: 23566315] |
| NCI-H460 | IC50 |
0.85 μM
Compound: 4, Oncrasin-1
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Cytotoxicity against human H460 cells after 72 hrs by MTT assay
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
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[PMID: 25874341] |
Oncrasin-1 (0.1-33 μM, 3 d) induces dose-dependent cytotoxicity in T29Kt1 cells (IC50 = 4.81 μM)[1].
Oncrasin-1 (31 nM-33 μM) effectively kills K-Ras-mutant H460, H2122, H2887, and A549 cells with an IC50 ≤ 3 μM[1].
Oncrasin-1 (1-10 μM, 12 h) increases the apoptotic cell percentages and leads to a substantial change in the subcellular localization of PKCι in both H460 and T29K1 cells[1].
Oncrasin-1 (33 nM-3.3 μM, 24 h) shows its cytotoxic effect in cancer cells (H460) is due to its induction of apoptosis in H460 cells[1].
Oncrasin-1 (1 μM, 12 h) shows that K-Ras is required to induce apoptosis[1].
Oncrasin-1 (1 μM, 4-12 h) markedly inhibits expression of luciferase in H460 and T27Kt1 cells but has no effect of only mild effect in T29 cells[2].
Oncrasin-1 (1 μM, 12 h) disrupts the interaction between PKCι and cyclin T1 and leads to transcription dysfunction in H460 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460 cells
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Concentration:33 nM, 100 nM, 330 nM, 1 μM, 3.3 μM
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Incubation Time:24 h
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Result:Activated caspase 3 and 8 effectively.
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Cell Line:H460, T29, T29Kt1
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Concentration:1 μM for H460, 10 μM for T29 and T29Kt1
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Incubation Time:12 h
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Result:Led to a dramatic suppression of phosphorylated RNA polymerase II and some SR proteins.
Reduced the phosphorylation of RNA polymerase II and SR proteins starting at 8 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 75629-57-1
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Appearance Solid
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분자량 269.73
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화학식 C16H12ClNO
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Color Light yellow to khaki
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SMILES
O=CC1=CN(CC(C=C2)=CC=C2Cl)C3=CC=CC=C31
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 100 mg/mL (370.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. 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. [Content Brief]
[2]. Guo W, 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7074 mL | 18.5371 mL | 37.0741 mL | 92.6853 mL |
| 5 mM | 0.7415 mL | 3.7074 mL | 7.4148 mL | 18.5371 mL | |
| 10 mM | 0.3707 mL | 1.8537 mL | 3.7074 mL | 9.2685 mL | |
| 15 mM | 0.2472 mL | 1.2358 mL | 2.4716 mL | 6.1790 mL | |
| 20 mM | 0.1854 mL | 0.9269 mL | 1.8537 mL | 4.6343 mL | |
| 25 mM | 0.1483 mL | 0.7415 mL | 1.4830 mL | 3.7074 mL | |
| 30 mM | 0.1236 mL | 0.6179 mL | 1.2358 mL | 3.0895 mL | |
| 40 mM | 0.0927 mL | 0.4634 mL | 0.9269 mL | 2.3171 mL | |
| 50 mM | 0.0741 mL | 0.3707 mL | 0.7415 mL | 1.8537 mL | |
| 60 mM | 0.0618 mL | 0.3090 mL | 0.6179 mL | 1.5448 mL | |
| 80 mM | 0.0463 mL | 0.2317 mL | 0.4634 mL | 1.1586 mL | |
| 100 mM | 0.0371 mL | 0.1854 mL | 0.3707 mL | 0.9269 mL |
Oncrasin-1 Related Classifications
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