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C3249

CR8

≥95% (HPLC)

Synonym(s):

(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1, (R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine, C&R8

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About This Item

Empirical Formula (Hill Notation):
C24H29N7O
CAS Number:
294646-77-8
Molecular Weight:
431.53
NACRES:
NA.77
PubChem Substance ID:
329775030
UNSPSC Code:
12352200
MDL number:
MFCD18785641
Assay:
≥95% (HPLC)
Form:
powder
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Quality Segment

100

assay

≥95% (HPLC)

form

powder

color

off-white

solubility

DMSO: ≥10 mg/mL

storage temp.

2-8°C

SMILES string

CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c3ccccn3)c4ncn(C(C)C)c4n1

InChI

1S/C24H29N7O/c1-4-19(14-32)28-24-29-22(21-23(30-24)31(15-27-21)16(2)3)26-13-17-8-10-18(11-9-17)20-7-5-6-12-25-20/h5-12,15-16,19,32H,4,13-14H2,1-3H3,(H2,26,28,29,30)/t19-/m1/s1

InChI key

HOCBJBNQIQQQGT-LJQANCHMSA-N

Biochem/physiol Actions

CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. Acts as a molecular glue to induce cyclin K degradation.
CR8 is a potent inhibitor of CDK1/2/5/7/9.

Features and Benefits

This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000185928
0000185928
0000134363
0000134364
0000094554

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Articles

Cyclin-dependent Kinases (CDKs)

Review properties, activators and inhibitors, and available products for researching cyclin-dependent kinases (CDKs).

Global Trade Item Number

SKUGTIN
C3249-5MG04061832445250
C3249-25MG04061832445243