KB-0742 Dihydrochloride

Catalog No.S9901 Batch:S990101

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)
* <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. <a class="sref" href="#s_ref">[1]</a>

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

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.

Cell Assay:^{<a class="sref" href="#s_ref">[1]</a>}

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:^{<a class="sref" href="#s_ref">[1]</a>}

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.

References

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

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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.

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