KB-0742 Dihydrochloride

Catalog No.S9901 Batch:S990101

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Technical Data

Formula

C16H25N5.2ClH
Molecular Weight 360.33 CAS No. 2416874-75-2
Solubility (25°C)* In vitro DMSO 72 mg/mL (199.81 mM)
Water 72 mg/mL (199.81 mM)
Ethanol 72 mg/mL (199.81 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.72mg/ml Taking the 1 mL working solution as an example, add 50 μL of 14.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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>
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>

Protocol (from reference)

Cell Assay:

<sup><a class="sref" href="#s_ref">[1]</a></sup>
  • 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.
Animal Study:

<sup><a class="sref" href="#s_ref">[1]</a></sup>
  • 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.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.