[CAS NO. 2490599-18-1] GMB-475
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PRODUCTS SPECIFICATIONS [2490599-18-1]
Catalog
SLK-S8888
Brand
Selleck
CAS
2490599-18-1
DESCRIPTION [2490599-18-1]
Overview
| MDL | MFCD32220458 |
|---|---|
| Molecular Weight | 861.93 |
| Molecular Formula | C43H46F3N7O7S |
| SMILES | FC(F)(OC1=CC=C(C=C1)NC2=CC(C3=CC=C(C=C3)OCCOCC(N[C@H](C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)=NC=N2)F |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1602 mL | 5.8009 mL | 11.6019 mL |
| 5 mM | 0.2320 mL | 1.1602 mL | 2.3204 mL |
| 10 mM | 0.1160 mL | 0.5801 mL | 1.1602 mL |
| 50 mM | 0.0232 mL | 0.1160 mL | 0.2320 mL |
Description
GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets protein and recruit Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
In vitro
GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells.
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