NST-628 | RAF-MEK molecular glue | Probechem Biochemicals

Chemical Structure : NST-628

CAS No.: 3002056-30-3

加入收藏

NST-628 (NST628)

货号: 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.

规格	价格	库存
2 mg	￥2480	In stock
5 mg	￥3880	In stock
10 mg	￥5780	In stock
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

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.

物理化学性质&存储条件

分子量	488.47
分子式	C22H18F2N4O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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-

参考文献

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.

NST-628 (NST628)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

NST-628 (NST628)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.