An SHP-2 inhibitor
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GDC-1971

Item No. 39884

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(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
CAS Number
2377352-49-1
Synonyms
  • Migoprotafib
Molecular Formula
C25H26N8O
Formula Weight
454.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlMethanol: Sparingly soluble: 1-10 mg/ml
SMILES
N[C@@H]1C2=CC=CC=C2OC31CCN(CC3)C4=CN=C5C(N6C7=CC=CN=C7CCC6)=NNC5=N4
InChi Code
InChI=1S/C25H26N8O/c26-22-16-5-1-2-8-19(16)34-25(22)9-13-32(14-10-25)20-15-28-21-23(29-20)30-31-24(21)33-12-4-6-17-18(33)7-3-11-27-17/h1-3,5,7-8,11,15,22H,4,6,9-10,12-14,26H2,(H,29,30,31)/t22-/m1/s1
InChi Key
RGCGBFIARQENML-JOCHJYFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $702

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    25 mg

    $1,403

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    Cayman Chemical
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    Product Description

    GDC-1971 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = <0.001 µM).1 It is selective for SHP-2 over SHP-2 containing a glutamate-to-lysine substitution at position 76 (SHP-2E76K; IC50 = 0.17 µM). GDC-1971 reduces the levels of phosphorylated ERK in a reporter assay using KYSE-520 esophageal cancer cells (IC90 = 0.012 µM) and inhibits proliferation of the same cells (IC50 = 0.32 µM). In vivo, GDC-1971 (30 or 100 mg/kg two times per day) reduces tumor volume in KYSE-520 and NCI H358 non-small cell lung cancer (NSCLC) mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Taylor, A.M., Williams, B.R., Giordanetto, F., et al. Identification of GDC-1971 (RLY-1971), a SHP2 inhibitor designed for the treatment of solid tumors. J. Med. Chem. 66(19), 13384-13399 (2023).