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) .
For research use only. We do not sell to patients.
- CAS No.: 2621927-57-7
- Formula: C33H33FN6O2
- Molecular Weight:564.65
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
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) |
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.
Chemical Information
-
CAS No. 2621927-57-7
-
Appearance Solid
-
Molecular Weight 564.65
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
-
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)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRTX-EX185 Related Classifications
HY-145962 Related Classifications
Powered by Bioz