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(R)-CR8 (trihydrochloride)

Product Name
(R)-CR8 (trihydrochloride)
CAS No.
1786438-30-9
Chemical Name
(R)-CR8 (trihydrochloride)
Synonyms
(R)?-?CR8 triHCl;(R)-Isomer trihydrochloride;(R)?-?CR8 (trihydrochloride);CR8, (R)-Isomer trihydrochloride;(R)-CR8 trihydrochloride, 10 mM in DMSO;(R) CR8 trihydrochloride,(R)-CR-8 trihydrochloride,(R)CR8 trihydrochloride;(R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol trihydrochloride
CBNumber
CB65848911
Molecular Formula
C24H30ClN7O
Formula Weight
468
MOL File
1786438-30-9.mol
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(R)-CR8 (trihydrochloride) Property

storage temp. 
Store at -20°C
solubility 
DMSO: 62.5 mg/mL (115.54 mM)
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0107260
Product name
(R)-CR8trihydrochloride
Purity
99.02%
Packaging
5mg
Price
$150
Updated
2021/12/16
ChemScene
Product number
CS-0107260
Product name
(R)-CR8trihydrochloride
Purity
99.02%
Packaging
10mg
Price
$250
Updated
2021/12/16
ChemScene
Product number
CS-0107260
Product name
(R)-CR8trihydrochloride
Purity
99.02%
Packaging
50mg
Price
$1090
Updated
2021/12/16
ChemScene
Product number
CS-0107260
Product name
(R)-CR8trihydrochloride
Purity
99.02%
Packaging
100mg
Price
$1900
Updated
2021/12/16
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(R)-CR8 (trihydrochloride) Chemical Properties,Usage,Production

Uses

(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect[1][2]. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K[3].

in vivo

(R)-CR8 trihydrochloride (5?mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment[2].

Animal Model:Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330?g)[2]
Dosage:5?mg/Kg
Administration:i.p.
Result:Resulted in a significant reduction in lesion size.

IC 50

CDK1/cyclinB1: 0.09 μM (IC50); cdk2/cyclin A: 0.072 μM (IC50); CDK2/cyclinE: 0.041 μM (IC50); Cdk5/p25: 0.11 μM (IC50); CDK7/cyclin H: 1.1 μM (IC50); CDK9/Cyclin T: 0.18 μM (IC50); CK1δ/ε: 0.4 μM (IC50)

storage

Store at +4°C

References

[1] Bettayeb K, et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008 Oct 2;27(44):5797-807. DOI:10.1038/onc.2008.191
[2] Kabadi SV, et al. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13. DOI:10.1038/jcbfm.2013.228
[3] S?abicki M, et al. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K [published online ahead of print, 2020 Jun 3]. Nature. 2020;10.1038/s41586-020-2374-x. DOI:10.1038/s41586-020-2374-x

(R)-CR8 (trihydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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(R)-CR8 (trihydrochloride) Suppliers

China 32 United States 5 Global 37
BOC Sciences
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1786438-30-9, (R)-CR8 (trihydrochloride)Related Search:


  • (R)?-?CR8 (trihydrochloride)
  • CR8, (R)-Isomer trihydrochloride
  • (R)?-?CR8 triHCl
  • (R)-Isomer trihydrochloride
  • (R) CR8 trihydrochloride,(R)-CR-8 trihydrochloride,(R)CR8 trihydrochloride
  • (R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol trihydrochloride
  • (R)-CR8 trihydrochloride, 10 mM in DMSO
  • 1786438-30-9