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BSJ-4-116

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Purity:99.09%

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COA HNMR HPLC

BSJ-4-116

Catalog No. T9117Cas No. 2519823-34-6

BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).

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Pack Size	Price	Availability
1 mg	$62	In Stock
5 mg	$133	In Stock
10 mg	$226	In Stock
25 mg	$490	In Stock
50 mg	$723	In Stock
100 mg	$987	In Stock
1 mL x 10 mM (in DMSO)	$198	In Stock

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Product Introduction

Bioactivity

Description

In vitro

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.BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-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.

Chemical Properties

Molecular Weight	837.38
Formula	C40H49ClN8O8S
Cas No.	2519823-34-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (298.55 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.1942 mL	5.9710 mL	11.9420 mL	59.7100 mL
5 mM	0.2388 mL	1.1942 mL	2.3884 mL	11.9420 mL
10 mM	0.1194 mL	0.5971 mL	1.1942 mL	5.9710 mL
20 mM	0.0597 mL	0.2986 mL	0.5971 mL	2.9855 mL
50 mM	0.0239 mL	0.1194 mL	0.2388 mL	1.1942 mL
100 mM	0.0119 mL	0.0597 mL	0.1194 mL	0.5971 mL

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In Vivo Formulation Calculator (Clear solution)

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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