GMB-475 free base · Synonyms: 2489876-37-9

GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance.

For research use only. Not for human or veterinary use.

Target PROTAC Bcr-Abl Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GMB-475 structure

CAS No.: 2490599-18-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 589.00	BP-02353-100mg	In stock	Get quote
250 mg	USD 989.00	BP-02353-250mg	In stock	Get quote
500 mg	USD 1,589.00	BP-02353-500mg	In stock	Get quote
1 g	USD 2,689.00	BP-02353-1g	In stock	Get quote
2 g	Inquire	BP-02353-2g	In stock	Inquire

Custom Size Bulk Inquiry

Description

GMB-475 is a degrader of BCR-ABL1 tyrosine kinase 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.

Biological activity

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

Identifiers

SMILES: FC(F)(F)OC1=CC=C(NC2=CC(C3=CC=C(OCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)C=C3)=NC=N2)C=C1
InChIKey: ONDVWISBMHHLGZ-SBJIGXGQSA-N

Specifications

MW (average): 861.9280
Formula: C₄₃H₄₆F₃N₇O₇S
CAS No.: 2490599-18-1
Physical state: Solid
Color: Light yellow to yellow
Shipping: 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: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, not in water

In vitro: DMSO : 250 mg/mL

Documents

References

[1]. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation. Cancer Res. 2019 Sep 15;79(18):4744-4753.

[2]. Ye W, et al. The proteolysis targeting chimera GMB-475 combined with dasatinib for the treatment of chronic myeloid leukemia with BCR::ABL1 mutants. Front Pharmacol. 2022 Oct 3;13:931772.

Same research area

Search Cancer