MedKoo Cat#: 130038 | Name: Migoprotafib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Migoprotafib
Migoprotafib
CAS#2377352-49-1

Theoretical Analysis

MedKoo Cat#: 130038

Name: Migoprotafib

CAS#: 2377352-49-1

Chemical Formula: C25H26N8O

Exact Mass: 454.2230

Molecular Weight: 454.54

Elemental Analysis: C, 66.06; H, 5.77; N, 24.65; O, 3.52

Price and Availability

Size Price Availability Quantity
5mg USD 950.00 2 Weeks
10mg USD 1,650.00 2 Weeks
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Related CAS #
No Data
Synonym
Migoprotafib; RLY-1971; RLY 1971; RLY1971; GDC-1971; GDC 1971; GDC1971;
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
InChi Key
RGCGBFIARQENML-JOCHJYFZSA-N
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
SMILES Code
N[C@H]1C2(CCN(C3=CN=C4C(NN=C4N5CCCC6=NC=CC=C56)=N3)CC2)OC7=CC=CC=C17
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 454.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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.