Home Cell Cycle CDK inhibitor KB-0742 Dihydrochloride For research use only.

KB-0742 Dihydrochloride

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

KB-0742 Dihydrochloride Chemical Structure

CAS No. 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

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

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
NCT04718675 Recruiting
Relapsed Solid Tumors|Refractory Solid Tumors|Non-Hodgkin Lymphoma
Kronos Bio
 February 8 2021 Phase 1|Phase 2

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

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


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In vivo
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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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