2. Cell Cycle/DNA Damage
  3. CDK
  4. PNU-292137

PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model.

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PNU-292137 Chemical Structure

PNU-292137 Chemical Structure

CAS No. : 326823-27-2

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PNU-292137 Related Antibodies

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Description

PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model[1].

IC50 & Target[1]

CDK2/cyclinA

37 nM (IC50)

CDK2/cyclin E

92 nM (IC50)

Cdk5/p25

114 nM (IC50)

CDK1/cyclinB

270 nM (IC50)

CDK4/cyclinD1

>10000 nM (IC50)

GSK-3β

1905 nM (IC50)

ERK-2

4600 nM (IC50)

Molecular Weight

291.35

Formula

C18H17N3O
CAS No.
SMILES

O=C(CC1=CC=C2C=CC=CC2=C1)NC3=NNC(C4CC4)=C3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PNU-292137 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PNU-292137326823-27-2PNU292137PNU 292137CDKCyclin dependent kinasehydrophobic pocketATP pocketproliferationcolonprostateInhibitorinhibitorinhibit

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