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Orantinib (SU6668) - 10mM in DMSO, high purity , CAS No.252916-29-3(DMSO), Inhibitor of epidermal growth factor receptor;Inhibitor of fibroblast growth factor receptor 1;Inhibitor of kinase insert domain receptor;Inhibitor of platelet derived growth factor receptor beta

COA COA
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Item Number
O407925
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O407925-1ml
1ml
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$153.90
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PDGFRβ Selective Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms TSU-68 | (Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of epidermal growth factor receptor;Inhibitor of fibroblast growth factor receptor 1;Inhibitor of kinase insert domain receptor;Inhibitor of platelet derived growth factor receptor beta
Product Description

Information

Orantinib (TSU-68, SU6668) has greatest potency againstPDGFRautophosphorylation withKiof 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does
In vitro

TSU-68 is a competitive inhibitor, with regard to ATP, to Flk-1/KDR trans-phosphorylation, FGFR1 trans-phosphorylation, and PDGFRβ kinases autophosphorylation. TSU-68 (0.03-10 μM) inhibits tyrosine phosphorylation of KDR in VEGF stimulated HUVECs. TSU-68 also inhibits PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ at a minimum concentration of 0.03-0.1 μM. TSU-68 inhibits acidic FGF-induced phosphorylation of the FGFR1 substrate 2 at 10 μM and higher. However, TSU-68 (up to 100 μM) has no effect on EGF-stimulated EGFR tyrosine phosphorylation in NIH-3T3 cells overexpressing EGFR. TSU-68 inhibits VEGF-driven and FGF-driven mitogenesis of HUVECs with mean IC50 of 0.34 μM and 9.6 μM, respectively. In human myeloid leukemia MO7E cells, TSU-68 inhibits the tyrosine autophosphorylation of stem cell factor (SCF) receptor, c-kit, with IC50 of 0.1-1 μM, as well as ERK1/2 phosphorylation, a signaling event downstream of c-kit activation. TSU-68 also inhibits SCF-induced proliferation of MO7E cells with IC50 of 0.29 μM, and induces apoptosis.

In vivo

TSU-68 (75-200 mg/kg) induces tumor growth inhibition against a broad range of tumor types in xenograft models in athymic mice, including A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells. TSU-68 (75 mg/kg) also suppresses tumor angiogenesis of C6 glioma xenografts. In a tumor model of HT29 human colon carcinoma, TSU-68 (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core. TSU-68 promotes abnormal stromal development at the periphery of carcinomas. In a rabbit VX2 liver tumor model, TSU-68 (200 mg/kg) augments the effect of chemotherapeutic infusion.
Cell Data

cell lines：MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562 cells and et al.

Concentrations：0.03-10 μM , dissolved in DMSO as 10 mM stock solution

Incubation Time：1 hour (before ligand stimulation)

Powder Purity:≥99%

Product Properties

Ki Data PDGFRβ, Ki: 8 nM

Associated Targets(Human)

EGFR Tclin Epidermal growth factor receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FGFR1 Tclin Fibroblast growth factor receptor 1 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
TNIK Tchem TRAF2 and NCK-interacting protein kinase (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDGFRB Tclin Platelet-derived growth factor receptor beta (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
BMPR2 Tchem Bone morphogenetic protein receptor type-2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles CC1=C(CCC(O)=O)C(=C([NH]1)/C=C/2C(=O)NC3=CC=CC=C23)C
Molecular Weight 310.35

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro Water: 50 mg/mL (200.0 mM); DMSO: Insoluble; Ethanol: Insoluble;

Solution Calculators

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