SU-9516

CAS No. 377090-84-1

SU-9516( SU9516 | SU 9516 )

Catalog No. M14301 CAS No. 377090-84-1

A selective CDK2 inhibitor with IC50 of 22 nM; shows less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK; decreases the phosphorylation of pRb, and increases caspase-3 activation.

A selective CDK2 inhibitor with IC50 of 22 nM; shows less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK; decreases the phosphorylation of pRb, and increases caspase-3 activation.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 39 In Stock
5MG 60 In Stock
10MG 95 In Stock
25MG 197 In Stock
50MG 356 In Stock
100MG 530 In Stock
500MG 1152 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    SU-9516
  • Note
    Research use only, not for human use.
  • Brief Description
    A selective CDK2 inhibitor with IC50 of 22 nM; shows less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK; decreases the phosphorylation of pRb, and increases caspase-3 activation.
  • Description
    A selective CDK2 inhibitor with IC50 of 22 nM; shows less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK; decreases the phosphorylation of pRb, and increases caspase-3 activation.
  • In Vitro
    SU9516 shows slight activities against PKC, p38, PDGFr and EGFR, with IC50 of >10, >10, 18, and >100 μM. SU9516 (5 μM) decreases cdk2-specific Phosphorylation of pRB and inhibits cell cycle progression in RKO cells. SU9516 (5 μM) also induces apoptosis in RKO and SW480 Cells. SU9516 (5 μM) results in enhanced pRb/E2F complex formation in HT-29 cells. SU9516 enhances presence of E2F species in multiprotein complexes. SU9516 (5 μM) rapidly induces cytochrome crelease, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1. SU9516 causes down-regulation of Mcl-1 mRNA levels in human leukemia cells. Furthermore, SU9516 treatment results in a marked increase in reactive oxygen species production.
  • In Vivo
    ——
  • Synonyms
    SU9516 | SU 9516
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CDK1|CDK2|CDK4|p38|PKC
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    377090-84-1
  • Formula Weight
    241.2453
  • Molecular Formula
    C13H11N3O2
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C1NC2=C(C=C(OC)C=C2)/C1=C/C3=CN=CN3
  • Chemical Name
    2H-Indol-2-one, 1,3-dihydro-3-(1H-imidazol-5-ylmethylene)-5-methoxy-, (3Z)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Lane ME, et al. Cancer Res. 2001 Aug 15;61(16):6170-7. 2. Gao N, et al. Mol Pharmacol. 2006 Aug;70(2):645-55. 3. Sarathy A, et al. Mol Ther. 2017 Apr 5. pii: S1525-0016(17)30121-1.
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