NST-628

CAS: 3002056-30-3 F: C22H18F2N4O5S W: 488.46

NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 al

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Bioactivity	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].
Invitro	NST-628 (100 nM; 2 h)在 BRAF 类 II/III 突变细胞模型中展现出比其他 RAF 和 MEK 抑制剂更高的抗增殖活性，且不促进 BRAF 和 CRAF 的异二聚体形成[2]。NST-628 (4-100 nM; 48 h) 在 NRAS 突变型 IPC-298和 SK-MEL-2，NF1突变型 MeWo 和 KRAS 突变型 HCT116细胞系中，以剂量依赖性方式增加早期和晚期凋亡细胞的水平并减少活细胞[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NST-628 相关抗体: Apoptosis Analysis[2] Cell Line:
In Vivo	qd：每天 1 次；b.i.d:每天 2 次NST-628 (p.o.; 3 mg/kg; qd, 5 mg/kg; qd 或 1.5 mg/kg; b.i.d) 在带 KRAS 和 NRAS 突变的肿瘤模型中显著减缓了肿瘤的生长。在 SK-MEL-2-luc 模型中导致肿瘤消退[2]。NST-628 (i.g.; 0.3-3 mg/kg; qd; 18-20 天) 在小鼠中能够以剂量依赖性方式抑制 RAS-MAPK 途径。在 MeWo-luc 模型中有较强的抗肿瘤活性[2]。NST-628 (i.g.; 2 mg/kg; qd; 26 天) 在 NCI-H23-KRASG12C 突变型肺腺癌模型中，减缓肿瘤生长。有效抑制 RAS–MAPK 途径[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	3002056-30-3
Formula	C22H18F2N4O5S
Molar Mass	488.46
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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