All AbMole products are for research use only, cannot be used for human consumption.
Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner.
J Pharm Biomed Anal. 2021 Dec 30;211:114562.
Method Development and Validation for Simultaneous Determination of Six Tyrosine Kinase Inhibitors and Two Active Metabolites in Human Plasma Using UPLC–MS/MS for Therapeutic Drug Monitoring
Sunitinib purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | RS4;11, MV4;11, and OC1-AML5 |
| Preparation method | Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3. |
| Concentrations | Dissolved in DMSO, final concentrations ~10 μM |
| Incubation time | 24 and 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors |
| Formulation | Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution |
| Dosages | ~80 mg/kg |
| Administration | Orally once daily |
| Molecular Weight | 398.47 |
| Formula | C22H27FN4O2 |
| CAS Number | 557795-19-4 |
| Solubility (25°C) | 25 mg/mL warmed in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
|---|
| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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