MRTX-EX185
MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC50 of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC50s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) .
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2621927-57-7
- Formel: C33H33FN6O2
- Molecular Weight:564.65
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
KRas G12D 90 nM (IC50) |
K-Ras WT 110 nM (IC50) |
KRas G12C 290 nM (IC50) |
KRas G12V 700 nM (IC50) |
KRAS G13D 240 nM (IC50) |
KRas Q61H 130 nM (IC50) |
In Vitro
MRTX-EX185 (0.1 nM-100 μM) suppresses cell proliferation (IC50 = 70 nM) in KRAS (G12D)-driven SW-1990 pancreatic cancer cells, and is non-toxic to non-KRAS-dependent cell lines (HEK293 cells)[1].
MRTX-EX185 (1 nM-100 μM) significantly inhibits ERK phosphorylation (p-ERK) in KRAS(G12C)-driven cell lineages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
CAS. Nr. 2621927-57-7
-
Appearance Solid
-
Molecular Weight 564.65
-
Formel C33H33FN6O2
-
Color Light brown to brown
-
SMILES
OC1=CC(C2=C(F)C3=NC(OCC45CCCN4CCC5)=NC(N6C[C@@](N7)([H])CC[C@@]7([H])C6)=C3C=N2)=C8C(C#C)=CC=CC8=C1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MRTX-EX185 Related Classifications
HY-145962 Related Classifications
Powered by Bioz