RAS GTPase-IN-3
RAS GTPase-IN-3 is a RAS GTPase inhibitor that targets multiple KRAS-Q61 mutant variants. RAS GTPase-IN-3 binds to the switch II pocket of GTP-bound KRAS-Q61R, positions its side-chain imidazole group near the GTP γ-phosphate, and accelerates GTP hydrolysis of KRAS-Q61. RAS GTPase-IN-3 inhibits Sos-catalyzed nucleotide exchange on GTP-bound KRAS. RAS GTPase-IN-3 only activates GTP hydrolysis of HRAS-Q61R/Q95H and NRAS-Q61R/L95H mutant proteins. RAS GTPase-IN-3 can be applied in research related to cancers driven by KRAS-Q61 mutations.
For research use only. We do not sell to patients.
- Formula: C37H35F3N8O2
- Molecular Weight:680.72
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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]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
KRas Q61H |
In Vitro
RAS GTPase-IN-3 (compound 1) potently activates GTP hydrolysis in the previously catalytically inactive KRAS-Q61R protein; it selectively activates GTP hydrolysis in the tested oncogenic KRAS Q61X mutants, and exhibits no GTP hydrolysis-stimulating activity against native wild-type KRAS, KRAS-G12D, HRAS-Q61R, or NRAS-Q61R[1].
RAS GTPase-IN-3 directly binds to the vicinity of the nucleotide phosphate group on KRAS-Q61R, which is consistent with the phenomenon of occupying the switch-II pocket near the GTP γ-phosphate[1].
RAS GTPase-IN-3 drives a time-dependent transformation of GTP bound to KRAS-Q61R to produce GDP and inorganic phosphate within 10 h at a 2:1 molar ratio of compound to protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 680.72
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Formula C37H35F3N8O2
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SMILES
FC1=C(N=C(OC[C@@]23N(CCC3)C[C@H](F)C2)N=C4N5C[C@H]6N(CC7=CNC=N7)[C@H](CC6)C5)C4=CN=C1C8=C(C(C#C)=C(F)C=C9)C9=CC(O)=C8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RAS GTPase-IN-3 Related Classifications
HY-189129 Related Classifications
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