GMB 475, CAS 2490599-18-1

Formulation: A solid

Formal Name: (4R)-3-methyl-N-[2-[2-[4-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]phenoxy]ethoxy]acetyl]-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide

Purity: ≥98%

Formula Markup: C43H46F3N7O7S

Formula Weight: 861,9

Shelf life (days): 1460

CAS Number: 2490599-18-1

Notes: GMB 475 is a proteolysis-targeting chimera (PROTAC) containing the Bcr-Abl inhibitor GNF-5 (Item No. 16254) conjugated to VHL ligand 1 (Item No. 21591).{49846} It induces degradation of Bcr-Abl with a half-maximal degradation concentration (DC50) value of 340 nM. GMB 475 selectively inhibits the proliferation of K562 chronic myeloid leukemia (CML) and Bcr-Abl-expressing Ba/F3 cells (IC50 = ~1 µM for both) over parental Ba/F3 cells (IC50 = >10 µM). It also inhibits the proliferation of Ba/F3 cells expressing mutant Bcr-Abl (IC50s = 1.98 and 0.37 µM for Bcr-AblT315I and Bcr-AblG250E, respectively). GMB 475 (2.5 µM) induces apoptosis in primary human CML cells.

• SKU: CAY40463-5
• Manufacturer: Cayman Chemical
• Manufacturer SKU: 40463-5
• Package Unit: 5 mg
• Quantity Unit: STK