(R)-CR8 trihydrochloride

Catalog No.E0647 Batch:E064701

Technical Data

Formula	C₂₄H₂₉N₇O.₃ClH
Molecular Weight	540.92	CAS No.	1786438-30-9
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (184.87 mM)
		Water	100 mg/mL (184.87 mM)
		Ethanol	25 mg/mL (46.21 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

(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

(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]

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]

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[3]}	Animal Models lateral fluid percussion-induced traumatic brain injury rats(male; Sprague-Dawley) Dosages 5 mg/Kg Administration i.p.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[3]}

Animal Models
lateral fluid percussion-induced traumatic brain injury rats(male; Sprague-Dawley)
Dosages
5 mg/Kg
Administration
i.p.

References

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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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