Oncrasin-1

Catalog No.S0780 Batch:S078001

Print

Technical Data

Formula

C16H12ClNO
Molecular Weight 269.73 CAS No. 75629-57-1
Solubility (25°C)* In vitro DMSO 54 mg/mL (200.2 mM)
Ethanol 13 mg/mL (48.19 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 2.7mg/ml (10.01mM) Taking the 1 mL working solution as an example, add 50 μL of 54 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.39mg/ml (1.45mM) Taking the 1 mL working solution as an example, add 50 μL of 7.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. This compound drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
Targets
K-ras [2] RNA polymerase II [1] PKCι [2]
In vitro Oncrasin-1 (NSC-743380) 是一种选择性细胞毒性化合物，对携带特定 KRAS 基因突变的肺癌细胞具有显著效果。该化合物通过诱导细胞周期阻滞和促进凋亡来抑制肿瘤细胞增殖。研究显示，这种化学物质对正常细胞的毒性较低，表明其具有良好的选择性。进一步的机制研究表明，该化合物可能通过调节 RAS 信号通路下游效应分子发挥作用。实验证明，这种化学物质的抗肿瘤活性与其浓度和处理时间呈正相关。此外，该化合物在动物模型中亦展现出良好的耐受性和抑制肿瘤生长的效果。因此，这种化学物质有望成为治疗 KRAS 突变型肺癌的潜在药物候选物。
In vivo Oncrasin-1 (NSC-743380) 是一种选择性抗肿瘤小分子，通过诱导癌细胞凋亡发挥作用。该化合物最初在针对KRAS突变型肺癌细胞的筛选中被发现，能有效抑制多种癌细胞系的增殖。研究表明，这种化学物质的作用机制涉及对RNA聚合酶I的抑制，从而导致核仁应激和细胞周期阻滞。进一步的实验证实，该分子对正常细胞影响较小，显示出良好的治疗窗口。目前，这种小分子已成为研究靶向癌症治疗的重要工具化合物。

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/21443218/
  • https://pubmed.ncbi.nlm.nih.gov/18794128/

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.