Oncrasin-1

Cat. No.: HY-16662 Purity: 98.28%: FAQs
Data Sheet SDS COA Handling Instructions

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Oncrasin-1 Chemical Structure

CAS No. : 75629-57-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 143	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 143	In-stock	Estimated Time of Arrival: December 31
Solid
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 122	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 224	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 410	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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K-Ras H-Ras N-Ras Ras

Biological Activity
Purity & Documentation
References
Customer Review

Description

Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells. IC50 value: 1.0 μM(A549, K-ras 12H and p53 Wt) [1] Target: human lung cancer cells with K-Ras mutation; K-Ras/PKCiota pathway inhibitor in vitro: effectively kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. The cytotoxic effects correlated with apoptosis inductionas was evidenced by increase of apoptotic cells and activation of caspase-3 and caspase-8 upon the treatment of oncrasin-1 in sensitive cells. Treatment with oncrasin-1 also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells. Furthermore, oncrasin-1 induced apoptosis was blocked by siRNA of K-Ras or PKCι suggesting that oncrasin-1 is targeted to a novel K-Ras/PKCι pathway [1]. oncrasin-1 treatment led to coaggregation of PKCiota and splicing factors into megaspliceosomes but had no obvious effects on the DNA repair molecule Rad51. Moreover, oncrasin-1 treatment suppressed the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells but not in resistant cells [2]. in vivo: The in vivo administration of oncrasin-1 suppressed the growth of K-ras mutant human lung tumor xenografts by >70% and prolonged the survival of nude mice bearing these tumors, without causing detectable toxicity [1].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	≤ 3 μM Compound: 5	Cytotoxicity against human A549 cells by SRB assay Cytotoxicity against human A549 cells by SRB assay	[PMID: 23566315]
A549	IC₅₀	2.48 μM Compound: 4, Oncrasin-1	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25874341]
HT-29	IC₅₀	1.71 μM Compound: 4, Oncrasin-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25874341]
MDA-MB-231	IC₅₀	26.1 μM Compound: 4, Oncrasin-1	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	[PMID: 25874341]
NCI-H2122	IC₅₀	≤ 3 μM Compound: 5	Cytotoxicity against human NCI-H2122 cells by SRB assay Cytotoxicity against human NCI-H2122 cells by SRB assay	[PMID: 23566315]
NCI-H460	IC₅₀	≤ 3 μM Compound: 5	Cytotoxicity against human H460 cells by SRB assay Cytotoxicity against human H460 cells by SRB assay	[PMID: 23566315]
NCI-H460	IC₅₀	0.25 μM Compound: oncrasin-1	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	[PMID: 21443218]
NCI-H460	IC₅₀	0.85 μM Compound: 4, Oncrasin-1	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25874341]

Molecular Weight

269.73

Formula

C₁₆H₁₂ClNO

CAS No.

75629-57-1

Appearance

Solid

Color

Light yellow to khaki

SMILES

O=CC1=CN(CC(C=C2)=CC=C2Cl)C3=CC=CC=C31

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (9.27 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.28%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (254 KB) LCMS (272 KB)

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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oncrasin-175629-57-1Oncrasin1Oncrasin 1RasApoptosisInhibitorinhibitorinhibit

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Oncrasin-1

Oncrasin-1 Related Antibodies

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Complete Stock Solution Preparation Table

Oncrasin-1 Related Classifications

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