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(R)​-​CR8

Names

[ CAS No. ]:
294646-77-8

[ Name ]:
(R)​-​CR8

[Synonym ]:
(2R)-2-[(9-Isopropyl-6-{[4-(2-pyridinyl)benzyl]amino}-9H-purin-2-yl)amino]-1-butanol
3ddp
CR-8
HMS3229B13
1-Butanol, 2-[[9-(1-methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-, (2R)-

Biological Activity

[Description]:

(R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 (CR8) 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 (CR8) induces apoptosis and has neuroprotective effect[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

[Target]

Cdk1/cyclin B: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)


[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.

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
671.4±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H29N7O

[ Molecular Weight ]:
431.533

[ Flash Point ]:
359.8±34.3 °C

[ Exact Mass ]:
431.243347

[ PSA ]:
100.78000

[ LogP ]:
2.10

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.664

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Precursor & DownStream

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Related Compounds