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Chemical Structure| 377090-84-1 Chemical Structure| 377090-84-1

Structure of SU9516
CAS No.: 377090-84-1

Chemical Structure| 377090-84-1

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SU9516 is a selective and potent CDK2 inhibtor with IC50 of 22 nM, less potent for CDK1/CDK4 (IC50=40/200 nM), and with no inhibition on PKC, EGFR, p38MAPK, etc.

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Product Details of SU9516

CAS No. :377090-84-1
Formula : C13H11N3O2
M.W : 241.25
SMILES Code : O=C1NC2=C(C=C(OC)C=C2)/C1=C/C3=CNC=N3
MDL No. :MFCD17010284
InChI Key :QNUKRWAIZMBVCU-WCIBSUBMSA-N
Pubchem ID :5289419

Safety of SU9516

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SU9516

Hedgehog

Isoform Comparison

Biological Activity

Target
  • CDK4

    CDK4, IC50:200 nM

  • CDK2

    CDK2, IC50:22 nM

  • CDK1

    CDK1, IC50:40 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
CDK2 0.13 μM SU9516 is an ATP-competitive inhibitor of CDK2 with an IC50 value of 0.13 μM PMC3098941
MV4-11 500 nM 72 h Evaluate the apoptotic effect of SU9516 in combination with ABT-737 and AKTi-1/2 on MV4-11 cells, showing significant increase in apoptosis PMC10058112
Human DMD patient myotubes 0.1 μM SU9516 increased levels of α7β1 integrin and inhibited the SPAK/OSR1 kinase pathway PMC6417831
K562 cells 5 μM 24 hours SU9516 significantly enhanced the sensitivity of K562 cells to MTX, with significant growth inhibition at 0.05 μM MTX or higher concentrations. PMC11158204
CCRF-CEM cells 5 μM 24 hours SU9516 significantly enhanced the sensitivity of CCRF-CEM cells to MTX, with significant growth inhibition at 0.05 μM MTX or higher concentrations. PMC11158204
Jurkat cells 2 μM 6, 12, 24 hours SU9516 started to decrease DHFR mRNA expression after 6 hours and DHFR protein levels after 12 hours. PMC11158204
Jurkat cells 1, 2, 5, 10 μM 24 to 72 hours SU9516 significantly inhibited the growth of Jurkat cells in a dose-dependent manner. After 72 h, cell growth was inhibited to 56%, 31%, 17%, and 9% of controls by SU9516 at 1, 2, 5, and 10 μM, respectively. PMC11158204
Kasumi-1 500 nM 72 h Evaluate the apoptotic effect of SU9516 in combination with ABT-737 and AKTi-1/2 on Kasumi-1 cells, showing significant increase in apoptosis PMC10058112
VMCF-7DNp53 cells 5 μM Inhibited cdk2 activity, preventing centriole reduplication and centrosome amplification in vMCF-7DNp53 cells PMC2526020
Human normal foreskin skin fibroblast primary cells (CRL-2097) 10 μM 1 day Convert fibroblasts into induced oligodendrocyte-like cells (iOLCs) expressing oligodendrocyte-specific marker O4. PMC8997971
SUM149PT cells 1 µM SU9516 combined with 0.5 µM paclitaxel 72 hours To evaluate the cytotoxic effect of SU9516 combined with paclitaxel, showing that the combination significantly enhanced apoptosis. PMC4121417
SUM149PT cells 1 µM 72 hours To evaluate the cytotoxic effect of SU9516 on CD44+/CD24-/Low CSCs, showing that CD44+/CD24-/Low CSCs were highly sensitive to SU9516. PMC4121417
VMCF-7DNp53/Aurora-A cells 1 µM 48 h Inhibition of Cdk2 activity reduces Aurora-A centrosomal localization and suppresses centrosome amplification PMC3658847
VMCF-7DNp53 cells 1 µM 48 h Inhibition of Cdk2 activity reduces Aurora-A centrosomal localization and suppresses centrosome amplification PMC3658847

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57/BL6 mice Cuprizone-induced demyelination model Direct injection into the corpus callosum 100 μM Single injection, lasting 2 weeks Test the ability of the chemical cocktail to promote remyelination in vivo, showing significantly higher remyelination levels in the chemical cocktail injection group compared to the PBS control group. PMC8997971
Mdx mice Duchenne muscular dystrophy model Oral gavage 5mg/kg Daily from 3 to 10 weeks of age SU9516 treatment significantly improved weight gain, forelimb grip strength, diaphragm function, and reduced fibrosis PMC6417831

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.15mL

0.83mL

0.41mL

20.73mL

4.15mL

2.07mL

41.45mL

8.29mL

4.15mL

References

 

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