SR 3029 – 10 mg

Brand:
Cayman
CAS:
1454585-06-8
Storage:
-20
UN-No:
Non-Hazardous - /

SR 3029 is an inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 44 and 260 nM, respectively).{47522} It is selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models.{47523} It reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue.  

 

Available on backorder

SKU: 27048 - 10 mg Category:

Description

An inhibitor of CK1δ and CK1ε (IC50s = 44 and 260 nM, respectively); selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by >90% at 10 µM; inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 (IC50s = 576, 368, 428, 427, and 3,000 nM, respectively); inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM); reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models at 20 mg/kg per day; reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue


Formal name: N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-9H-purin-6-amine

Synonyms: 

Molecular weight: 480.5

CAS: 1454585-06-8

Purity: ≥98%

Formulation: A solid


Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Kinase Inhibitors|CK1||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|Casein Kinase Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling