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BSJ-03-204

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Catalog No. T30600Cas No. 2349356-09-6
Alias BSJ03204

BSJ-03-204 is a rationally designed PROTAC composed of cereblon and CDK ligands that functions as a potent and selective palbociclib-based CDK4/6 dual degrader, achieving nanomolar inhibition of CDK4/D1 and CDK6/D1 complexes without inducing IKZF1/3 degradation, BSJ-03-204 exhibit strong anticancer activity with improved selectivity.

BSJ-03-204

BSJ-03-204

😃Good
Catalog No. T30600Alias BSJ03204Cas No. 2349356-09-6
BSJ-03-204 is a rationally designed PROTAC composed of cereblon and CDK ligands that functions as a potent and selective palbociclib-based CDK4/6 dual degrader, achieving nanomolar inhibition of CDK4/D1 and CDK6/D1 complexes without inducing IKZF1/3 degradation, BSJ-03-204 exhibit strong anticancer activity with improved selectivity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$81735 days35 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
BSJ-03-204 is a rationally designed PROTAC composed of cereblon and CDK ligands that functions as a potent and selective palbociclib-based CDK4/6 dual degrader, achieving nanomolar inhibition of CDK4/D1 and CDK6/D1 complexes without inducing IKZF1/3 degradation, BSJ-03-204 exhibit strong anticancer activity with improved selectivity.
Targets&IC50
CDK4-CyclinD1:26.9 nM, CDK6-CyclinD1:10.4 nM
In vitro
In wild-type cells, treatment with BSJ-03-204 (0.1-5 μM) for 4 hours induced the rapid degradation of CDK4/6 without affecting IKZF1/3 levels. In Mantle Cell Lymphoma (MCL) cell lines, the compound demonstrated potent anti-proliferative activity across a broad concentration range (0.0001-100 μM) over 3 to 4 days [1].
SynonymsBSJ03204
Chemical Properties
Molecular Weight832.9
FormulaC43H48N10O8
Cas No.2349356-09-6
SmilesO=C(NCCCCN1CCN(C2=CN=C(C=C2)NC=3N=CC4=C(N3)N(C(=O)C(C(=O)C)=C4C)C5CCCC5)CC1)COC6=CC=CC=7C(=O)N(C(=O)C67)C8C(=O)NC(=O)CC8
Relative Density.1.397 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (96.05 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.2006 mL6.0031 mL12.0062 mL60.0312 mL
5 mM0.2401 mL1.2006 mL2.4012 mL12.0062 mL
10 mM0.1201 mL0.6003 mL1.2006 mL6.0031 mL
20 mM0.0600 mL0.3002 mL0.6003 mL3.0016 mL
50 mM0.0240 mL0.1201 mL0.2401 mL1.2006 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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