Art. -Nr.: HY-16662

Oncrasin-1

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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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Reinheit: 98.16%
CAS. Nr.: 75629-57-1
Formel: C₁₆H₁₂ClNO
Molecular Weight:269.73

Speicherung:

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

Oncrasin-1 Chemical Structure

CAS. Nr.: 75629-57-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RNA Polymerase

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Alle Ras Isoform-spezifische Produkte anzeigen :

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	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	≤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	0.85 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]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

H460 cells
Concentration:

33 nM, 100 nM, 330 nM, 1 μM, 3.3 μM
Incubation Time:

24 h
Result:

Activated caspase 3 and 8 effectively.

Western Blot Analysis^[2]

Cell Line:

H460, T29, T29Kt1
Concentration:

1 μM for H460, 10 μM for T29 and T29Kt1
Incubation Time:

12 h
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.

In Vivo

Oncrasin-1 (100 mg/kg, i.p., daily for 10 days) suppresses tumor growth by 75.4% and leads to prolonged survival in nude mice inoculated with H460 cells into the dorsal flank^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 75629-57-1
Appearance Solid
Molecular Weight 269.73
Formel C₁₆H₁₂ClNO
Color Light yellow to khaki
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Oncrasin-1

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Cell Cycle/DNA Damage Compound Library

GPCR/G Protein Compound Library

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Cell Death Library

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MCE Bioactive Compound Library

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Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Oncrasin-1 Related Classifications

HY-16662 Related Classifications