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GMB-475

Catalog No. T8488 CAS 2490599-18-1

GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein

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GMB-475, CAS 2490599-18-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 88.00
5 mg	In stock	$ 210.00
10 mg	In stock	$ 369.00
25 mg	In stock	$ 622.00
50 mg	In stock	$ 885.00
100 mg	In stock	$ 1,190.00
500 mg	In stock	$ 2,430.00
1 mL * 10 mM (in DMSO)	In stock	$ 289.00

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Purity: 100%

Purity: 98.78%

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Description

In vitro

GMB-475 inhibited the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitized Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells.?Reverse phase protein array analysis suggested additional differences in levels of phosphorylated SHP2, GAB2, and SHC associated with BCR-ABL1 degradation.?Importantly, GMB-475 reduced viability and increased apoptosis in primary CML CD34+ cells, with no effect on healthy CD34+ cells at identical concentrations.?GMB-475 degraded BCR-ABL1 and reduced cell viability in primary CML stem cells.?Together, these findings suggest that combined BCR-ABL1 kinase inhibition and protein degradation may represent a strategy to address BCR-ABL1-dependent drug resistance, and warrant further investigation into the eradication of persistent leukemic stem cells, which rely on neither the presence nor the activity of the BCR-ABL1 protein for survival.

Molecular Weight	861.93
Formula	C43H46F3N7O7S
CAS No.	2490599-18-1

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (110.22 mM), Sonification is recommended.

References and Literature

1. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. Cancer Res. 2019 Jul 16. pii: canres.1236.2019.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Angiogenesis related Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Bioactive Compound Library Ubiquitination Compound Library

Related Products

Related compounds with same targets

Imatinib impurities3 AG957 Dasatinib Nocodazole BGG463 AD57 Multi-kinase inhibitor 1 SKLB 1028

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Keywords

GMB-475 2490599-18-1 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl PROTACs Apoptosis Inhibitor inhibit GMB475 GMB 475 inhibitor

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