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Oncrasin-1 DNA/RNA Synthesis inhibitor

Name: Oncrasin-1
Brand: Selleck Chemicals
SKU: S0780
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0780

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.

Chemical Structure

Molecular Weight: 269.73

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S078001 DMSO]54 mg/mL]false]Ethanol]13 mg/mL]false]Water]Insoluble]false Purity: 99.8%

99.8

Related Targets	CDK Microtubule Associated Ras HSP (HSP90) PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
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Chemical Information, Storage & Stability

Molecular Weight	269.73	Formula	C₁₆H₁₂ClNO	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	75629-57-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C=O

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (200.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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 1 40%PEG300 2 5%Tween80 3 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 1 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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Mechanism of Action

Targets/IC₅₀/Ki	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。
References	[1] https://pubmed.ncbi.nlm.nih.gov/21443218/ [2] https://pubmed.ncbi.nlm.nih.gov/18794128/

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