Home Cell Cycle CDK inhibitor (R)-CR8 trihydrochloride For research use only.

(R)-CR8 trihydrochloride

(R)-CR8 trihydrochloride, one of CR8 isomers, is a potent inhibitor CDK1/2/5/7/9 with antiproliferative effect and proapoptotic effect on CML cell lines.

(R)-CR8 trihydrochloride Chemical Structure

(R)-CR8 trihydrochloride Chemical Structure

CAS: 1786438-30-9

Purity & Quality Control

Batch: E064701 DMSO] 100 mg/mL] false] Water] 100 mg/mL] false] Ethanol] 25 mg/mL] false Purity: 99.08%
99.08

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Signaling Pathway

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Biological Activity

Description (R)-CR8 trihydrochloride, one of CR8 isomers, is a potent inhibitor CDK1/2/5/7/9 with antiproliferative effect and proapoptotic effect on CML cell lines.
Targets
CDK1 [1] CDK2 [1] CDK5 [1] CDK7 [1] CDK9 [1]
In vitro
In vitro

(R)-CR8 trihydrochloride (0.1-100 μM) is a potent inducer of apoptotic cell death with an IC50 of 0.49 μM for SH-SY5Y cell line. (R)-CR8 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.[2]
Cell Research Cell lines SH-SY5Y cell line
Concentrations 0.1-100 μM, 0.25-10 μM
Incubation Time 48 h
Method

(R)-CR8 trihydrochloride treatment is performed on exponentially growing cultures(0.1-100 μM or 0.25-10 μM; 48h). Control experiments are carried also using appropriate dilutions of DMSO. Cell viability is determined by measuring the reduction of MTS. Cell death is determined by measuring the level of LDH activity released upon cell lysis.The expression level of PARP is tested by western blotting.
In Vivo
In vivo

(R)-CR8 trihydrochloride treatment attenuates sensorimotor and cognitive deficits, alleviates depressive-like symptoms, and decreased lesion volume in lateral fluid percussion-induced traumatic brain injury rats.[3]
Animal Research Animal Models lateral fluid percussion-induced traumatic brain injury rats(male; Sprague-Dawley)
Dosages 5 mg/Kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 540.92 Formula

C24H29N7O.3ClH
CAS No. 1786438-30-9 SDF --
Smiles Cl.Cl.Cl.CCC(CO)NC1=NC(=C2N=C[N](C(C)C)C2=N1)NCC3=CC=C(C=C3)C4=CC=CC=N4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (184.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 25 mg/mL


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In vivo
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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.

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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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