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Pan-RAS-IN-6
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Catalog No. T89850
Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.
Pan-RAS-IN-6
Pan-RAS-IN-6
😃Good
Catalog No. T89850
Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 10 mg | Inquiry | Backorder | |
| 50 mg | Inquiry | Backorder |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively. |
| Targets&IC50 | KRas G12V:0.3 nM, KRas G12C:1.3 nM, KRas G12D:4.7 nM |
| In vitro | Pan-RAS-IN-6 inhibits cell proliferation in NCI-H23, NCI-H358, NCI-H2444, RKN, and SW620 with IC50 values of 0.17 nM, 0.12 nM, 0.17 nM, 0.045 nM, and 0.1 nM, respectively. The compound demonstrates IC50 values against KRAS G12V, wild-type KRAS, wild-type HRAS, and wild-type NRAS-BRAF with CYPA interaction of 7 nM, 32 nM, 38 nM, and 35 nM, respectively; and in conditions of G12C, G12D, and G12V, the IC50 values for KRAS-BRAF with CYPA interaction are 9.7 nM, 49.5 nM, and 7.1 nM. Additionally, Pan-RAS-IN-6 inhibits pERK with IC50 values of less than 0.6 nM for G12C and G12V, and 0.9 nM for G12D. |
| In vivo | Pan-RAS-IN-6, administered orally at a dose of 30 mg/kg once daily, inhibits tumor growth and promotes tumor regression in a mouse model of non-small cell lung cancer (NSCLC) brain tumors. Additionally, this compound reduces the expression of DUSP6 in the brains of the NCI-H1373-Luc model. |
| Molecular Weight | 837.08 |
| Formula | C46H60N8O5S |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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