Home Angiogenesis PROTAC chemical - Bcr-Abl chemical - E3 Ligase chemical GMB-475 For research use only.

GMB-475

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.

GMB-475 Chemical Structure

GMB-475 Chemical Structure

CAS: 2490599-18-1

Purity & Quality Control

Batch: Purity: 99.58%
99.58

Related compound libraries

Choose Selective PROTAC Inhibitors

Biological Activity

Description 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 [1] E3 ligase [1]
In vitro
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.[1]
Cell Research 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
Method

Cell viability assay: Cell lines and patient samples are exposed to dose ranges of GMB-475 (0.001-0.300 μM) and incubated for 3 days at 37°C, 5% CO2 and subjected to a CellTiter 96 AQueous One solution cell proliferation assay. Reverse phase protein arrays (RPPA): K562 cells are treated with DMSO, GMB-475 (5 μM) for 8 h in duplicate, washed twice with PBS and lysed in RPPA lysis buffer.

Chemical lnformation & Solubility

Molecular Weight 861.93 Formula

C43H46F3N7O7S
CAS No. 2490599-18-1 SDF --
Smiles CC1=C(SC=N1)C2=CC=C(CNC(=O)C3CC(O)CN3C(=O)C(NC(=O)COCCOC4=CC=C(C=C4)C5=CC(=NC=N5)NC6=CC=C(OC(F)(F)F)C=C6)C(C)(C)C)C=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (116.01 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy GMB-475 | GMB-475 supplier | purchase GMB-475 | GMB-475 cost | GMB-475 manufacturer | order GMB-475 | GMB-475 distributor