Migoprotafib

SKU: orb1687245

Description

Migoprotafib (GDC-1971) is a potent, selective SHP2 phosphatase inhibitor used in cancer research. It is applied in studies of advanced solid tumors, enabling both in vitro biochemical assays and in vivo efficacy models to investigate RTK and MAPK pathway signaling.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 2377352-49-1
• MW: 454.53
• Purity: 99.16% (May vary between batches)
• Formula: C₂₅H₂₆N₈O
• SMILES: N[C@H]1C2(OC=3C1=CC=CC3)CCN(CC2)C=4N=C5C(=NC4)C(=NN5)N6C=7C(CCC6)=NC=CC7
• Target: p38 MAPK,Phosphatase,ERK
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (7.26 mM);DMSO:80 mg/mL (176.01 mM)

Bioactivity

• In Vivo:
  In mouse xenograft models, Migoprotafib (30–60 mg/kg, oral gavage, once daily) showed strong antitumor efficacy, particularly in combination with KRAS G12C inhibitors (e.g., GDC-6036), resulting in complete or substantial tumor regression (treatment up to 21 days).
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• In Vitro:
  Migoprotafib is a selective SHP2 inhibitor that demonstrates potent antiproliferative activity in various tumor cell lines (e.g., NCI-H358, KYSE520, and LoVo). In vitro, Migoprotafib (0.001–10 μM, 2–6 days) alone or in combination with KRAS G12C inhibitors (e.g., GDC-6036) significantly suppressed pERK levels and induced cell cycle arrest, indicating effective MAPK pathway inhibition.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GDC1971, GDC-1971, RG 6433, RLY-1971, RO-7517834

Compound Identifiers

PubChem CID

139512018