Art. -Nr.: HY-138188

KRA-533

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

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Reinheit: 98.73%
CAS. Nr.: 10161-87-2
Formel: C₁₃H₁₆BrNO₃
Molecular Weight:314.18

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

KRA-533 Chemical Structure

CAS. Nr.: 10161-87-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

KRAS^[1]

Alle Ras Isoform-spezifische Produkte anzeigen :

In Vitro

KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent^[1].
? KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death^[1].
? KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCC827 cells
Concentration:

10 μM
Incubation Time:

48 hours
Result:

Enhanced KRAS activity to a greater extent.

Apoptosis Analysis^[1]

Cell Line:

H157 cells
Concentration:

0~15 μM
Incubation Time:

48 hours
Result:

Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.

In Vivo

KRA-533 (0~30 mg/kg; i.p.; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner^[1].
? KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses^[1].

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

Animal Model:

Nu/Nu nude mice (mutant KRAS xenografts)^[1]
Dosage:

0~30 mg/kg
Administration:

i.p.; 28 days
Result:

Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner.

Chemical Information

CAS. Nr. 10161-87-2
Appearance Solid
Molecular Weight 314.18
Formel C₁₃H₁₆BrNO₃
Color Off-white to light brown
SMILES

O=C(O)C1=CC=C(CCCCNC(CBr)=O)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Proc Natl Acad Sci U S A

Pan-ErbB inhibition impairs cognition via disrupting myelination and aerobic glycolysis in oligodendrocytes. [Abstract]

2024 Nov 5;121(45):e2405152121. PMID: 39475641
Cell Signal

ARTN drives ABCB1-mediated chemoresistance in gastric cancer cells by promoting ELK4 phosphorylation. [Abstract]

2026 Oct:146:112668. PMID: 42285190

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (795.72 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

3.1829 mL

15.9144 mL

31.8289 mL

5 mM

0.6366 mL

3.1829 mL

6.3658 mL

10 mM

0.3183 mL

1.5914 mL

3.1829 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Xu K, et al. Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy [published correction appears in Mol Cancer. 2020 May 20;19(1):93]. Mol Cancer. 2019;18(1):85. Published 2019 Apr 10. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1829 mL	15.9144 mL	31.8289 mL	79.5722 mL
	5 mM	0.6366 mL	3.1829 mL	6.3658 mL	15.9144 mL
	10 mM	0.3183 mL	1.5914 mL	3.1829 mL	7.9572 mL
	15 mM	0.2122 mL	1.0610 mL	2.1219 mL	5.3048 mL
	20 mM	0.1591 mL	0.7957 mL	1.5914 mL	3.9786 mL
	25 mM	0.1273 mL	0.6366 mL	1.2732 mL	3.1829 mL
	30 mM	0.1061 mL	0.5305 mL	1.0610 mL	2.6524 mL
	40 mM	0.0796 mL	0.3979 mL	0.7957 mL	1.9893 mL
	50 mM	0.0637 mL	0.3183 mL	0.6366 mL	1.5914 mL
	60 mM	0.0530 mL	0.2652 mL	0.5305 mL	1.3262 mL
	80 mM	0.0398 mL	0.1989 mL	0.3979 mL	0.9947 mL
	100 mM	0.0318 mL	0.1591 mL	0.3183 mL	0.7957 mL

Keywords

KRA-533

2 Cited Publications

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KRA-533

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Anti-Lung Cancer Compound Library

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Bioactive Compound Library Max

MCE Bioactive Compound Library

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High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) KRA-533

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KRA-533

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) KRA-533

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KRA-533 Related Classifications

HY-138188 Related Classifications