Pan-RAS-IN-6
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 3054023-07-0
- Formula: C46H60N8O5S
- Molecular Weight:837.08
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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KRas G12C 1.3 nM (IC50) |
KRas G12D 4.7 nM (IC50) |
KRas G12V 0.3 nM (IC50) |
Pan-RAS-IN-6 inhibits the proliferation of NCI-H23, NCI-H358, NCI-H2444, RKN, and SW620 cells with IC50of 0.17 nM, 0.12 nM, 0.17 nM, 0.045 nM, and 0.1 nM[1].
Pan-RAS-IN-6 with the IC50 values against KRAS G12V, wild-type KRAS, wild-type HRAS, wild-type NRAS-BRAF, and CYPA interactions are 7 nM, 32 nM, 38 nM, and 35 nM, respectively; under G12C, G12D, and G12V conditions, the IC50 values for the KRAS-BRAF and CYPA interaction are 9.7 nM, 49.5 nM, and 7.1 nM, respectively; when inhibiting pERK, the IC50 values for both G12C and G12V are less than 0.6 nM, while for G12D, the IC50 is 0.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pan-RAS-IN-6 (30 mg/kg, p.o., once daily) reduces the expression of DUSP6 in the brain of the NCI-H1373-Luc model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3054023-07-0
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Molecular Weight 837.08
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Formula C46H60N8O5S
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SMILES
O=C(OCC(C)(C)CC1=[C@@]([C@@]2=C([C@@H](OC)C)N=CC(N3CCN(C)CC3)=C2)N4C5=C1C=C6C=C5CCC4)[C@H]7NN(C([C@@H](NC([C@H]8[C@H](C)[C@@H]8C)=O)CC9=NC6=CS9)=O)CCC7
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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)
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