2. GPCR/G Protein MAPK/ERK Pathway Metabolic Enzyme/Protease
  3. Ras Phosphatase
  4. 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.

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Pan-RAS-IN-6 Chemical Structure

Pan-RAS-IN-6 Chemical Structure

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Pan-RAS-IN-6 Related Antibodies

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Description

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[1].

IC50 & Target

KRas G12C

1.3 nM (IC50)

KRas G12D

4.7 nM (IC50)

KRas G12V

0.3 nM (IC50)

In Vitro

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 Related Antibodies
In Vivo

Pan-RAS-IN-6 (30 mg/kg, oral, once daily) inhibits non-small cell lung cancer tumor growth and promoted tumor regression in a brain tumor mouse model[1].
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.

Animal Model: NSCLC MB mouse[1]
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); daily
Result: Made T/C 0.52% and TGI 104.68%.
Animal Model: NCI-H1373-Luc mouse[1]
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); daily
Result: Decrease the expression of DUSP6.
Molecular Weight

837.08

Formula

C46H60N8O5S
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Pan-RAS-IN-6 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pan-RAS-IN-6RasPhosphatasePan-RASMAPKG12CG12DG12VInhibitorinhibitorinhibit

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