ChemicalBook > CAS DataBase List > GMB-475

GMB-475

Product Name: GMB-475
CAS No.: 2490599-18-1
Chemical Name: GMB-475
Synonyms: GMB-475;GMB-475 ，S8888;GMB-475, 10 mM in DMSO;Bcr-Abl,GMB-475,PROTACs,GMB 475,Apoptosis,Inhibitor,inhibit,GMB475;(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-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CBNumber: CB58379743
Molecular Formula: C43H46F3N7O7S
Formula Weight: 861.94
MOL File: 2490599-18-1.mol

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GMB-475 Property

Boiling point:: 1029.7±65.0 °C(Predicted)
Density: 1.337±0.06 g/cm3(Predicted)
solubility: DMSO:145.4(Max Conc. mg/mL);168.69(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);58.01(Max Conc. mM)
form: Solid
pka: 13.50±0.46(Predicted)
color: Light yellow to yellow
InChIKey: ONDVWISBMHHLGZ-XAYQSWBHNA-N
SMILES: C(N1C[C@H](O)C[C@H]1C(=O)NCC1C=CC(C2=C(N=CS2)C)=CC=1)(=O)[C@H](C(C)(C)C)NC(=O)COCCOC1C=CC(C2=NC=NC(NC3C=CC(OC(F)(F)F)=CC=3)=C2)=CC=1 |&1:3,6,24,r|

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Ambeed

Product number: A1235114
Product name: (2S,4R)-1-((S)-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
Purity: 98%
Packaging: 1mg
Price: $77
Updated: 2021/12/16

Ambeed

Product number: A1235114
Product name: (2S,4R)-1-((S)-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
Purity: 98%
Packaging: 5mg
Price: $153
Updated: 2021/12/16

Ambeed

Product number: A1235114
Product name: (2S,4R)-1-((S)-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
Purity: 98%
Packaging: 10mg
Price: $238
Updated: 2021/12/16

Ambeed

Product number: A1235114
Product name: (2S,4R)-1-((S)-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
Purity: 98%
Packaging: 25mg
Price: $309
Updated: 2021/12/16

Ambeed

Product number: A1235114
Product name: (2S,4R)-1-((S)-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
Purity: 98%
Packaging: 50mg
Price: $402
Updated: 2021/12/16

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GMB-475 Chemical Properties,Usage,Production

Description

GMB-475 acts as a degrader of BCR-ABL 1 tyrosine kinase and as a recruiter of the E3 ligase Von Hippel Lindau (VHL) resulting in ubiquitination and subsequent degradation of oncogenic fusion proteins.

Uses

GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007))[1][2].

Biological Activity

GMB-475, a BCR-ABL1 Inhibitor Based on PROTAC, Has the Potential to Overcome BCR-ABL1-Dependent Drug Resistance. In both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1, GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers. Notably, GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants. GMB-475 reduces viability and increases apoptosis in primary chronic myeloid leukemia CD34+ cells, with no effect on healthy CD34+ cells. Furthermore, GMB-475 degrades BCR-ABL1 and reduces cell viability in primary chronic myeloid leukemia stem cells.

in vivo

GMB-475 (5 mg/kg; once every two days; 10 days; i.p.) improves chronic myeloid leukemia in mice with BCR::ABL1 mutant by targeted degradation of BCR-ABL1b and combined with dasatinib (HY-10181)^[2].

Animal Model:	8-week-old Balb/c mice were injected with Ba/F3-MG-p210-Luc cells via tail vein to establish a chronic myeloid leukemia (CML) mouse model^[2].
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection (i.p.); once every two days; 10 days
Result:	Showed a trend of reducing the tumor burden and prolonging the survival of the CML mouse model.

IC 50

STAT5; VHL; Bcr-Abl

storage

Store at -20°C

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. DOI:10.1158/0008-5472.CAN-19-1236
[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. DOI:10.3389/fphar.2022.931772

GMB-475 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from GMB-475 manufacturers

Hubei Chuchang Biotech Co., Ltd.

Product: GMB-475 2490599-18-1
Price: US $0.00-0.00/mg
Min. Order: 1mg
Purity: 98%
Supply Ability: 100G
Release date: 2024-04-17

2490599-18-1, GMB-475Related Search:

(2S,4R)-1-((S)-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

GMB-475

Bcr-Abl,GMB-475,PROTACs,GMB 475,Apoptosis,Inhibitor,inhibit,GMB475

GMB-475, 10 mM in DMSO

(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

GMB-475 ，S8888

2490599-18-1

C43H46F3N7O7S