1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    PDGFR
    FGFR
  3. (Z)-Orantinib

(Z)-Orantinib (Synonyms: (Z)-SU6668; (Z)-TSU-68)

Cat. No.: HY-10517A Purity: 99.02%
Handling Instructions

(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. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

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

(Z)-Orantinib Chemical Structure

(Z)-Orantinib Chemical Structure

CAS No. : 210644-62-5

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Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 119 In-stock
Estimated Time of Arrival: December 31
Solid
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 Get quote
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Based on 1 publication(s) in Google Scholar

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Description

(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. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors[1][2].

IC50 & Target[2]

Flk-1/KDR

2.1 μM (IC50)

PDGFRβ

0.008 μM (IC50)

FGFR1

1.2 μM (IC50)

In Vitro

SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (Ki=2.1 μM), FGFR1 trans-phosphorylation (Ki=1.2 μM), and PDGFR autophosphorylation (Ki=0.008 μM)[1].
SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs[1].
SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC50s of 0.34 and 9.6 μM, respectively[1].

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

In Vivo

SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice[1].
SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice[1].
SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice[1].

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

Animal Model: Female athymic mice (BALB/c, nu/nu) were implanted A431 tumor cells[1]
Dosage: 4, 40, 75, 200 mg/kg
Administration: P.o. daily for 21 days
Result: Induced 97% growth inhibition against A431 tumor at the dose of 97%.
No mortality was observed in any treatment group.
Molecular Weight

310.35

Formula

C₁₈H₁₈N₂O₃

CAS No.
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 : 50 mg/mL (161.11 mM; Need ultrasonic)

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: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Product Name:
(Z)-Orantinib
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HY-10517A
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