Migoprotafib
Migoprotafib, also known as GDC-1971 and RLY-1971, is a SHP2 allosteric inhibitor. GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.
For research use only. We do not sell to patients.
Chemical Information
| Name | Migoprotafib |
|---|---|
| Iupac Chemical Name | (3R)-1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1Hpyrazolo[3,4-b]pyrazin-6-yl]-spiro[benzofuran-2(3H),4'-piperidin]-3-amine |
| Synonyms | Migoprotafib; RLY-1971; RLY 1971; RLY1971; GDC-1971; GDC 1971; GDC1971; |
| Molecular Formula | C25H26N8O |
| Molecular Weight | 454.53 |
| Smile | N[C@H]1C2(CCN(C3=CN=C4C(NN=C4N5CCCC6=NC=CC=C56)=N3)CC2)OC7=CC=CC=C17 |
| InChiKey | RGCGBFIARQENML-JOCHJYFZSA-N |
| InChi | 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 |
| CAS Number | 2377352-49-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Taylor AM, Williams BR, Giordanetto F, Kelley EH, Lescarbeau A, Shortsleeves K, Tang Y, Walters WP, Arrazate A, Bowman C, Brophy E, Chan EW, Deshmukh G, Greisman JB, Hunsaker TL, Kipp DR, Saenz Lopez-Larrocha P, Maddalo D, Martin IJ, Maragakis P, Merchant M, Murcko M, Nisonoff H, Nguyen V, Nguyen V, Orozco O, Owen C, Pierce L, Schmidt M, Shaw DE, Smith S, Therrien E, Tran JC, Watters J, Waters NJ, Wilbur J, Willmore L. Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors. J Med Chem. 2023 Sep 29. doi: 10.1021/acs.jmedchem.3c00483. Epub ahead of print. PMID: 37774359.
Chemical Structure
