BSJ-4-116

This product is for research use only, not for human use. We do not sell to patients.

BSJ-4-116
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250mg$1950Check With Us
500mg$3250Check With Us
1g$4875Check With Us

Cat #: V2485 CAS #: 2519823-34-6 Purity ≥ 99%

Description: BSJ-4-116 is a novel, potent and selective CDK12 degrader (PROTAC)( IC50 = 6 nM).

References: Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17(6):675-683.

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Molecular Weight (MW)837.38
Molecular FormulaC40H49ClN8O8S
CAS No.2519823-34-6
SMILES CodeO=C(NCCCCCCCN1C[C@H](NC2=NC=C(Cl)C(NC3=CC=CC=C3S(=O)(C(C)C)=O)=N2)CCC1)COC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O
SynonymsBSJ-4-116; BSJ4-116; BSJ 4-116; BSJ-4116; BSJ4116; BSJ 4116;
ProtocolIn VitroBSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein. BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-4-116 (50 nM; 6-24 hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line. BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.1942 mL5.9710 mL11.9420 mL23.8840 mL
5mM0.2388 mL1.1942 mL2.3884 mL4.7768 mL
10mM0.1194 mL0.5971 mL1.1942 mL2.3884 mL
20mM0.0597 mL0.2986 mL0.5971 mL1.1942 mL
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.