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) .
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- CAS No.: 2621927-57-7
- Formule: C33H33FN6O2
- Masse moléculaire:564.65
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Stockage:
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]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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
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CAS No. 2621927-57-7
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Appearance Solid
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Masse moléculaire 564.65
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Formule C33H33FN6O2
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Color Light brown to brown
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
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Fiche technique (273 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRTX-EX185 Related Classifications
HY-145962 Related Classifications
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