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Chemical Structure : GDC-1971
CAS No.: 2377352-49-1
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $228 | In stock | |
| 5 mg | $358 | In stock | |
| 10 mg | $548 | In stock | |
| 25 mg | Get quote | ||
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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).
| M.Wt | 454.54 | |
| Formula | C25H26N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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