Name: KB-0742 Dihydrochloride
Brand: Selleck Chemicals
SKU: S9901
Rating: 5 (1 reviews)

KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.

KB-0742 Dihydrochloride Chemical Structure

CAS: 2416874-75-2

Purity & Quality Control

Batch: S990101 DMSO] 72 mg/mL] false] Water] 72 mg/mL] false] Ethanol] 72 mg/mL] false Purity: 98.72%

98.72

KB-0742 Dihydrochloride Related Products

Related Targets	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	Click to Expand

Signaling Pathway

CDK Signaling Pathway

Choose Selective CDK Inhibitors

Biological Activity

Description

KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.

Targets

CDK9/cyclin T1 ^[1]

6 nM

In vitro
In vitro	KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs in 22Rv1 cells. <sup><a class="sref" href="#s_ref">[1]</a></sup>
Cell Research	Cell lines	22Rv1 cells
	Concentrations	0–40 μM
	Incubation Time	8 h
	Method	22Rv1 cells are plated in 96-well plates, adding 100 μL of a 75,000 cells/mL cell suspension in RPMI media (7,500 cells per well). After 24 h, cell culture media for 22Rv1 cells is removed and replaced with media containing 5 μM of IncuCyte® Caspase-3/7 Green Apoptosis Assay Reagent and either DMSO or KB-0742 dissolved in DMSO at the appropriate final concentration. Plates are then imaged over a period of 72 h.

In Vivo
In vivo	KB-0742 is a remarkably selective CDK9 inhibitor that leads to global downregulation of nascent transcription and AR-driven prostate cancer gene expression programs and displays in vivo efficacy in CRPC- and AML-derived xenograft models.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Animal Research	Animal Models	Male mus musculus (CB17-SCID,6-8 weeks, 18-22 g) inoculated with 22Rv1 tumor cells
	Dosages	3 mg/kg, 10 mg/kg, 30 mg/kg
	Administration	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04718675	Recruiting	Relapsed Solid Tumors\|Refractory Solid Tumors\|Non-Hodgkin Lymphoma	Kronos Bio	February 8 2021	Phase 1\|Phase 2

References

[1] André Richters, et al. Cell Chem Biol . 2021 Feb 18;28(2):134-147.e14.

Chemical Information & Solubility

Molecular Weight	360.33	Formula	C₁₆H₂₅N₅.₂ClH
CAS No.	2416874-75-2	SDF	--
Smiles	Cl.Cl.CCC(CC)C1=NC2=CC=N[N]2C(=C1)NC3CCC(N)C3
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 72 mg/mL ( (199.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 72 mg/mL

Ethanol : 72 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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

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% DMSO + % + % Tween 80 + % ddH₂O

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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
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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

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