Migoprotafib (GDC-1971, RLY-1971) | SHP2 inhibitor | Probechem Biochemicals

Chemical Structure : GDC-1971

CAS No.: 2377352-49-1

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GDC-1971 (Migoprotafib, GDC1971, RLY-1971, RLY1971)

货号: PC-20047Not For Human Use, Lab Use Only.

Migoprotafib (GDC-1971, RLY-1971) is a potent, selective, allosteric and orally bioavailable inhibitor of the non-receptor protein tyrosine phosphatase SHP2 (PTPN11), potently inhibits both wild-type SHP2 (IC50 <1 nM) and E76K activating mutant (IC50 < 250nM) in biochemical assays.

规格	价格	库存
5 mg	￥1980	In stock
10 mg	￥2980	In stock
25 mg	￥4980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Migoprotafib (GDC-1971, RLY-1971) is a potent, selective, allosteric and orally bioavailable inhibitor of the non-receptor protein tyrosine phosphatase SHP2 (PTPN11), potently inhibits both wild-type SHP2 (IC50 <1 nM) and E76K activating mutant (IC50 < 250nM) in biochemical assays.
GDC-1971 inhibits cellular proliferation in models harboring receptor tyrosine kinases (RTKs), SHP2, NF1, KRAS, or BRAF mutations in a dose-dependent manner.
GDC-1971 potently inhibits the proliferation of cellular models harboring KRAS G12C or G12A mutations (median IC50 <80 nM) compared to models harboring other KRAS G12, G13 or Q61 mutations (median IC50 >1 uM).
GDC-1971 demonstrates dose-dependent RAS/MAPK pathway inhibition and induces significant tumor-growth inhibition in human xenograft models harboring EGFR and KRAS alterations.
GDC-1971 demonstrates increased suppression of the MAPK signaling cascade and anti-proliferation synergy when combining with EGFR, ALK, and KRAS G12C inhibitors in vitro.
GDC-1971 exhibits dramatic synergic anti-tumor growth effects in vivo, when combining with the KRAS G12C covalent inhibitor GDC-6036 (Cat# PC-73323).

物理化学性质&存储条件

分子量	454.54
分子式	C25H26N8O
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	(3R)-1′-[3-(3,4-Dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]spiro[benzofuran-2(3H),4′-piperidin]-3-amine

参考文献

1. Bret Williams, et al. Discovery and characterization of the potent, allosteric SHP2 inhibitor GDC-1971 for the treatment of RTK/RAS driven tumors. Cancer Res (2022) 82 (12_Supplement): 3327.

GDC-1971 (Migoprotafib, GDC1971, RLY-1971, RLY1971)

生物&药学活性

物理化学性质&存储条件

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GDC-1971 (Migoprotafib, GDC1971, RLY-1971, RLY1971)

生物&药学活性

物理化学性质&存储条件

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