ChemicalBook CAS DataBase List 3002056-30-3

3002056-30-3

Name	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-
CAS	3002056-30-3
Molecular Formula	C22H18F2N4O5S
Molecular Weight	488.47
MOL File	3002056-30-3.mol

Chemical Properties

Boiling point	630.7±65.0 °C(predicted)
density	1.497±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
form	Solid
pka	6.60±0.50(predicted)
color	White to off-white

Hazard Information

Uses

NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors[1].

in vivo

qd: once daily ; b.i.d: twice daily
NST-628 (p.o.; 3 mg/kg; qd, 5 mg/kg; qd, or 1.5 mg/kg; b.i.d) can significantly slow tumor growth in mouse models with KRAS and NRAS mutations. NST-628 also leads to tumor regressions in the SK-MEL-2-luc model^[2].
NST-628 (i.g.; 0.3-3 mg/kg; qd; 18-20 days) inhibites the RAS-MAPK pathway in mice in a dose-dependent manner. NST-628 also exhibites strong antitumor activity in the MeWo-luc model^[2].
NST-628 (i.g.; 2 mg/kg; qd; 26 days) slows tumor growth and effectively inhibits the RAS–MAPK pathway in NCI-H23 KRASG12C-mutant lung adenocarcinoma model^[2].

Animal Model:	mouse models with KRAS and NRAS mutations ^[2]
Dosage:	3 mg/kg; qd, 5 mg/kg; qd, and 1.5 mg/kg; b.i.d
Administration:	p.o.
Result:	Significantly inhibited MEK and ERK phosphorylation in tumor tissues. Demonstrated superior anti-tumor efficacy and better tolerability than existing MEK inhibitors (e.g. Cobimetinib (HY-13064)) and RAF inhibitors (e.g. Belvarafenib (HY-109080)).

Animal Model:	NCI-H23 KRASG12C-mutant lung adenocarcinoma model ^[2]
Dosage:	2 mg/kg; 26 days
Administration:	i.g.; qd
Result:	The combination of NST-628 and sotorasib resulted in deep tumor regressions that were durable for the 40-day study duration.The combination led to a significant decrease in phospho-ERK levels.

References

[1] Ryan M B, et al. Abstract ND10: NST-628 is a novel, potent, fully brain-penetrant MAPK pathway molecular glue that inhibits RAS-and RAF-driven cancers[J]. Cancer Research, 2024, 84(7_Supplement): ND10-ND10.
[2] Meagan B et al. The Pan-RAF–MEK Nondegrading Molecular Glue NST-628 Is a Potent and Brain-Penetrant Inhibitor of the RAS–MAPK Pathway with Activity across Diverse RAS- and RAF-Driven Cancers. Cancer Discov 2024

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