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KB-0742 Dihydrochloride CDK inhibitor

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

Cat.No.S9901

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.

Chemical Structure

Molecular Weight: 360.33

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 98.72%

98.72

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Chemical Information, Storage & Stability

Molecular Weight	360.33	Formula	C₁₆H₂₅N₅.₂ClH	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2416874-75-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	Cl.Cl.CCC(CC)C1=NC2=CC=N[N]2C(=C1)NC3CCC(N)C3

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.720mg/ml (2.00mM)	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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.67mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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>
References	https://pubmed.ncbi.nlm.nih.gov/33086052/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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