This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
CDK/HDAC-IN-3
Catalog No. T78906 CAS
2944087-54-9
CDK/HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM, respectively. This compound is applicable in the treatment of acute myeloid leukemia (AML) [1].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
CDK/HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM, respectively. This compound is applicable in the treatment of acute myeloid leukemia (AML) [1].
In vitro
CDK/HDAC-IN-3 (compound 33a) at 1μM demonstrates potent and selective inhibition against CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM respectively [1]. At concentrations of 0.5 μM and 1.0 μM, this compound significantly induces differentiation of leukemia stem cell-like cells and inhibits the proliferation of AML [1]. Additionally, CDK/HDAC-IN-3 at 0.5 μM, 1.0 μM, and 2.0 μM markedly promotes differentiation of LSCs [1]. The compound also exhibits inhibitory effects on U937, HL-60, SKNO-1, and Kasumi-1 cells with IC50 values of 0.72 μM, 1.43 μM, 1.63 μM, and 0.89 μM respectively [1].
In vivo
CDK/HDAC-IN-3 (compound 33a), when administered intravenously (i.v.) or orally (p.o.) at doses of 5 mg/kg and 25 mg/kg, exhibits good oral bioavailability [1].
Molecular Weight
509.34
Formula
C24H18Cl2N6O3
CAS No.
2944087-54-9
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
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:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.