GMB-475 - 10mM in DMSO , CAS No.2490599-18-1

CAS: 2490599-18-1 Cat. No.: G492049 분자량: 861.93

GRADE & PURITY 10mM in DMSO

Synonyms

(2S)-1-((R)-3,3-dimethyl-2-(2-(2-(4-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide；(2S,4R)-1-((S)-3,3-Dimethyl-2-(2-(2-(4-(6-((4-(trifluorometho

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

Information

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.

Targets

BCR-ABL1 ; E3 ligase

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.

Cell Research(from reference)

Cell lines：K562 cell line, Ba/F3 murine cell lines (Ba/F3 BCR-ABL1 cells, Ba/F3 parental cells) 

Concentrations：0.001-0.300 μM, 5 μM 

Incubation Time：3 days, 8 h 

Specifications

동의어

(2S)-1-((R)-3,3-dimethyl-2-(2-(2-(4-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide；(2S,4R)-1-((S)-3,3-Dimethyl-2-(2-(2-(4-(6-((4-(trifluorometho

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

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.

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.

작업 유형

INHIBITOR

이름과 식별자

분자량

861.93

화학 및 물리적 특성

• 용해성: Solubility (25°C) In vitro DMSO: 100 mg/mL (116.01 mM); Ethanol: 50 mg/mL (58.0 mM); Water: Insoluble

자주 묻는 질문

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2490599-18-1, and the molecular weight is 861.93 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.