Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)-
- Product Name
- Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)-
- CAS No.
- 2377352-49-1
- Chemical Name
- Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)-
- Synonyms
- SHP-1971;GDC-1971;Migoprotafib;GDC-1971 (RLY-1971);Migoprotafib (GDC-1971);(R)-1'-(3-(3,4-Dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4'-piperidin]-3-amine;(R)-1'-(3-(3,4-Dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4'-piperidin]-3-amine;Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)-
- CBNumber
- CB610860058
- Molecular Formula
- C25H26N8O
- Formula Weight
- 454.54
- MOL File
- 2377352-49-1.mol
Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)- Property
- Boiling point:
- 714.1±60.0 °C(Predicted)
- Density
- 1.48±0.1 g/cm3(Predicted)
- solubility
- Acetonitrile: Slightly soluble: 0.1-1 mg/ml
Methanol: Sparingly soluble: 1-10 mg/ml - form
- Solid
- pka
- 9.52±0.50(Predicted)
- color
- Light yellow to yellow
- InChIKey
- RGCGBFIARQENML-ZEGQKUPANA-N
- SMILES
- N[C@@H]1C2=CC=CC=C2OC21CCN(C1=CN=C3C(N4CCCC5=NC=CC=C45)=NNC3=N1)CC2 |&1:1,r|
Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)- Chemical Properties,Usage,Production
Description
Migoprotafib is a protein tyrosine phosphate, also known as HPTP, inhibitor with potential as an antineoplastic agent.
Uses
Migoprotafib (GDC-1971) (compound 199) is a SHP2 inhibitor. Migoprotafib inhibits the MAPK/ERK signaling pathway, and exhibits antitumor activity[1][2].
in vivo
Migoprotafib (60 mg/kg, po for 28 days) exhibits antitumor efficacy in RIT1 xenograft mouse models[2].
| Animal Model: | RIT1 xenograft mouse models[2] |
| Dosage: | 60 mg/kg |
| Administration: | po for 28 days |
| Result: | Inhibited tumor growth. |
References
[1] Alexander M, et al. Shp2 phosphatase inhibitors and methods of use thereof. Patent WO2019183367A1.
[2] Maddalo D, et al. RIT1M90I is a driver of lung adenocarcinoma tumorigenesis and resistance to targeted therapy[J]. 2024.
[3] ALEXANDER M. TAYLOR*, LINDSAY WILLMORE Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors[J]. Journal of Medicinal Chemistry, 2023, 66 19: 13384-13399. DOI: 10.1021/acs.jmedchem.3c00483
Spiro[benzofuran-2(3H),4'-piperidin]-3-amine, 1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-, (3R)- Preparation Products And Raw materials
Raw materials
Preparation Products
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