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Chemical Structure : NST-628
CAS No.: 3002056-30-3
Catalog No.: PC-22122Not For Human Use, Lab Use Only.
NST-628 is a potent, brain-penetrant, pan-RAF-MEK molecular glue, prevents phosphorylation and activation of MEK by RAF, leading to deep durable inhibition of MEK kinase activity and downstream ERK signaling.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $248 | In stock | |
| 5 mg | $388 | In stock | |
| 10 mg | $578 | In stock | |
| 25 mg | Get quote | ||
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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NST-628 is a potent, brain-penetrant, pan-RAF-MEK molecular glue, prevents phosphorylation and activation of MEK by RAF, leading to deep durable inhibition of MEK kinase activity and downstream ERK signaling.
NST-628 engages all isoforms of RAF and prevents the formation of BRAF-CRAF heterodimers, a differentiated mechanism from all current RAF inhibitors.
NST-628 treatment glues ARAF, BRAF, and CRAF with unphosphorylated MEK1, stabilizing an inactive RAF-MEK complex and deeply inhibiting phospho-ERK signaling in MEK1 immunoprecipitation assay.
NST-628 demonstrates efficacy across multiple tumor types with RAS-MAPK alterations, including melanoma, lung, and pancreatic models.
NST-628 is broadly efficacious in models with BRAF Class II/III mutations, KRAS-mutations (G12C, G12D, G12V, G12R, Q61H), and NRAS-mutations (Q61x, G12x) as well as showing anti-proliferative effects in NF1-mutant/deficient models.
NST-628 (3-5 mg/kg QD treatment) led to tumor regressions in HCT116 (KRAS G13D colorectal) and IPC-298 (NRAS Q61L melanoma) xenograft models, 53% and 38% respectively, correlating to inhibition of both phospho-MEK and phospho-ERK in tumors.
NST-628 (3 mg/kg QD) dosing demonstrates broad anti-tumor responses across melanoma, lung, pancreatic, glioma, and ovarian models with patient derive xenograft (PDX) tumors harboring NF1, KRAS G12D/R, BRAF Class II/III, and NRAS Q61x mutations.
| M.Wt | 488.47 | |
| Formula | C22H18F2N4O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Sulfamide, N-[3-fluoro-4-[[7-[(3-fluoro-2-pyridinyl)oxy]-4-methyl-2-oxo-2H-1-benzopyran-3-yl]methyl]-2-pyridinyl]-N′-methyl- |
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1. Meagan B Ryan, et al. Mol Cancer Ther (2023) 22 (12_Supplement): A088.
2. Meagan B Ryan, et al. Mol Cancer Ther (2023) 22 (12_Supplement): A089.
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