1. Protein Tyrosine Kinase/RTK
  2. PDGFR
    VEGFR
    FGFR

Orantinib (Synonyms: SU6668; TSU-68)

Cat. No.: HY-10517 Purity: 99.02%
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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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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

Flt-1

2.1 μM (Ki)

PDGFRβ

0.008 μM (Ki)

FGFR1

1.2 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
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.
References
Cell Assay
[1]

Cells are seeded (3×105 cells/35-mm well) in DMEM containing 10% (v/v) FBS and grow to confluence and then quiesced in DMEM containing 0.1% serum for 2 hours before drug treatment. HUVECs (seeded at 2×106 cells/10-cm plate) are grown to confluence in endothelial cell growth media and then quiesced in endothelial cell basal media containing 0.5% FBS for 24 hours before drug treatment. All cell lines are incubated with Orantinib for 1 hour before ligand stimulation (100 ng/mL) for 10 min.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Colo205 and H460 cells are cultured in RPMI 1640 supplemented with 10% FBS and 2 mm glutamine. SKOV3 cells are passaged five times through mice to yield SKOV3TP5 cells. These cells are cultured in DMEM supplemented with 10% FBS and 2 mm glutamine. Tumor cells (3-10×106 cells/animal) are implanted s.c. into the hind flank of mice on day 0. Daily treatment with Orantinib or vehicle commenced 1 day after implantation of cells (to test efficacy against newly implanted tumors) or when tumors have reached a predetermined average size (to test efficacy against established tumors). Orantinib is delivered i.p. by bolus injection in DMSO or p.o. by gavage in a cremophor-based vehicle according to the specifics stated in figure and table legends. Tumor growth is measured twice a week using vernier calipers for the duration of treatment. Tumor volumes are calculated.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Orantinib
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Orantinib

Cat. No.: HY-10517