1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. PDGFR
    FGFR
    VEGFR
    Apoptosis
  3. Orantinib

Orantinib (Synonyms: SU6668; TSU-68)

Cat. No.: HY-10517 Purity: 98.80%
Handling Instructions

Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

For research use only. We do not sell to patients.

Orantinib Chemical Structure

Orantinib Chemical Structure

CAS No. : 252916-29-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg USD 756 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

IC50 & Target

PDGFRβ

8 nM (Ki)

FGFR1

1.2 μM (Ki)

Flt-1

2.1 μM (Ki)

In Vitro

Orantinib (SU6668; 0.03-10 μM) shows inhibitory activity against tyrosine phosphorylation of KDR in VEGF stimulated HUVECs, and also blocks PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ. Orantinib (≥10 μM) inhibits acidic FGF-induced phosphorylation of the FGFR1 substrate 2. However, Orantinib (up to 100 μM) has no effect on EGF-stimulated EGFR tyrosine phosphorylation in NIH-3T3 cells overexpressing EGFR. Furthermore, Orantinib inhibits VEGF-driven and FGF-driven mitogenesis of HUVECs with mean IC50 of 0.34 μM and 9.6 μM, respectively[1]. In human myeloid leukemia MO7E cells, Orantinib (SU6668) 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. In addition, Orantinib suppresses SCF-induced proliferation of MO7E cells with an IC50 of 0.29 μM, and induces apoptosis[2].

In Vivo

Orantinib (SU6668; 75-200 mg/kg) causes tumor growth inhibition on several tumor types in xenograft models in athymic mice, such as A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells. Orantinib (75 mg/kg) also inhibits tumor angiogenesis of C6 glioma xenografts[1]. In a tumor model of HT29 human colon carcinoma, Orantinib (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core. Orantinib enhances abnormal stromal development at the periphery of carcinomas[3]. Moreover, Orantinib (TSU-68; 200 mg/kg) augments the effect of chemotherapeutic infusion in a rabbit VX2 liver tumor model[4].

Clinical Trial
Molecular Weight

310.35

Formula

C₁₈H₁₈N₂O₃

CAS No.

252916-29-3

SMILES

CC1=C(/C=C2C3=CC=CC=C3NC/2=O)NC(C)=C1CCC(O)=O

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
In Vitro: 

DMSO : ≥ 28 mg/mL (90.22 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2222 mL 16.1108 mL 32.2217 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 mL
10 mM 0.3222 mL 1.6111 mL 3.2222 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

OrantinibSU6668 TSU-68SU 6668SU-6668TSU68TSU 68TSU-68PDGFRFGFRVEGFRApoptosisPlatelet-derived growth factor receptorFibroblast growth factor receptorVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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Orantinib
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