2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis Stem Cell/Wnt JAK/STAT Signaling Epigenetics
  3. PROTACs Bcr-Abl Apoptosis STAT JAK
  4. GMB-475

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)).

For research use only. We do not sell to patients.

GMB-475 Chemical Structure

GMB-475 Chemical Structure

CAS No. : 2490599-18-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 199 In-stock
Solution
10 mM * 1 mL in DMSO USD 199 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 210 In-stock
25 mg USD 380 In-stock
50 mg USD 560 In-stock
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Based on 1 publication(s) in Google Scholar

GMB-475 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].
IC50 & Target[1][2].

STAT5

 

VHL

 

Bcr-Abl

 

In Vitro

GMB-475 (0.01-100 μM, 3 days) inhibits leukemic stem cell viability in chronic myeloid leukemia (CML) by targeting degradation of BCR-ABL1 protein kinase and inhibiting downstream STAT5 biomarkers[1].
GMB-475 (0-5 μM, 48 h) blocks multiple molecules in the JAK-STAT pathway, blocks the cell cycle and promotes apoptosis in Ba/F3 cells harboring the BCR::ABL1 mutant[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GMB-475 Related Antibodies

Cell Viability Assay[1].

Cell Line: Human K562 cells and murine BCR-ABL1 transformed Ba/F3 cells
Concentration: 0.01-100 μM
Incubation Time: 3 days
Result: Inhibited the proliferation of two types of cells, with an IC50 value of approximately 1 μM.

Cell Viability Assay[2].

Cell Line: Ba/F3-MIG-p210 cells carrying BCR::ABL1T315I+F486S mutations
Concentration: 0-5 μM
Incubation Time: 48 h
Result: Exhibited a growth inhibition effect on Ba/F3-MIG-p210 cells carrying BCR::ABL1T315I+F486S mutations, with an IC50 value of 4.49 µM.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

861.93

Formula

C43H46F3N7O7S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (290.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1602 mL 5.8009 mL 11.6019 mL
5 mM 0.2320 mL 1.1602 mL 2.3204 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 6.25 mg/mL (7.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 6.25 mg/mL (7.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1602 mL 5.8009 mL 11.6019 mL 29.0047 mL
5 mM 0.2320 mL 1.1602 mL 2.3204 mL 5.8009 mL
10 mM 0.1160 mL 0.5801 mL 1.1602 mL 2.9005 mL
15 mM 0.0773 mL 0.3867 mL 0.7735 mL 1.9336 mL
20 mM 0.0580 mL 0.2900 mL 0.5801 mL 1.4502 mL
25 mM 0.0464 mL 0.2320 mL 0.4641 mL 1.1602 mL
30 mM 0.0387 mL 0.1934 mL 0.3867 mL 0.9668 mL
40 mM 0.0290 mL 0.1450 mL 0.2900 mL 0.7251 mL
50 mM 0.0232 mL 0.1160 mL 0.2320 mL 0.5801 mL
60 mM 0.0193 mL 0.0967 mL 0.1934 mL 0.4834 mL
80 mM 0.0145 mL 0.0725 mL 0.1450 mL 0.3626 mL
100 mM 0.0116 mL 0.0580 mL 0.1160 mL 0.2900 mL
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GMB-475 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GMB-4752490599-18-1GMB475GMB 475PROTACsBcr-AblApoptosisSTATJAKJanus kinasePROTACBCR-ABL1chronic myeloid leukemiaInhibitorinhibitorinhibit

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