[CAS NO. 377090-84-1] SU9516
PRODUCTS SPECIFICATIONS [377090-84-1]
DESCRIPTION [377090-84-1]
Overview
| MDL | MFCD17010284 |
|---|---|
| Molecular Weight | 241.25 |
| Molecular Formula | C13H11N3O2 |
| SMILES | O=C1NC2=C(C=C(OC)C=C2)/C1=C/C3=CN=CN3 |
4 Publications Citing Use of MCE
Summary
IC50 & Target
|
CDK2 22 nM (IC 50 ) |
CDK1 40 nM (IC 50 ) |
CDK4 200 nM (IC 50 ) |
PDGFr 18000 nM (IC 50 ) |
In Vitro
SU9516 shows slight activities against PKC, p38, PDGFr and EGFR, with IC 50 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 [1] . SU9516 (5 μM) results in enhanced pRb/E2F complex formation in HT-29 cells. SU9516 enhances presence of E2F species in multiprotein complexes [2] . 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 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 414.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.1451 mL | 20.7254 mL | 41.4508 mL |
| 5 mM | 0.8290 mL | 4.1451 mL | 8.2902 mL |
| 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 3.25 mg/mL (13.47 mM); Clear solution
References
- [1] Lane ME, et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7.
- [2] Yu B, et al. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem Pharmacol. 2002 Oct 1;64(7):1091-100.
- [3] Gao N, et al. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism. Mol Pharmacol. 2006 Aug;70(2):645-55.