Cat. No.: HY-10517A

(Z)-Orantinib

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

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(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.

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Pureté: 99.44%
CAS No.: 210644-62-5
Formule: C₁₈H₁₈N₂O₃
Masse moléculaire:310.35

Stockage:

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

(Z)-Orantinib Chemical Structure

CAS No.: 210644-62-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[2]

Flk-1/KDR

2.1 μM (IC₅₀)

PDGFRβ

0.008 μM (IC₅₀)

FGFR1

1.2 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform PDGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
3T3	IC₅₀	1 μM Compound: 5b	Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation	[PMID: 12646019]
HUVEC	IC₅₀	>50 μM Compound: SU-6668	Inhibition of rhFGF2-induced cellular proliferation of HUVEC Inhibition of rhFGF2-induced cellular proliferation of HUVEC	[PMID: 17618113]
HUVEC	IC₅₀	>50 μM Compound: SU-6668	Inhibition of rhFGF2-induced HUVEC proliferation Inhibition of rhFGF2-induced HUVEC proliferation	[PMID: 19110422]
HUVEC	IC₅₀	3.9 μM Compound: 51	Inhibition of VEGFR2 phosphorylation in HUVEC by chemiluminescence assay Inhibition of VEGFR2 phosphorylation in HUVEC by chemiluminescence assay	[PMID: 20403700]
MV4-11	IC₅₀	3.9 μM Compound: Orantinib	Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 29935772]
NIH3T3	IC₅₀	0.1 μM Compound: 51	Inhibition of PDGF-stimulated PDGFRbeta phosphorylation expressed in mouse NIH/3T3 cells by chemiluminescence assay Inhibition of PDGF-stimulated PDGFRbeta phosphorylation expressed in mouse NIH/3T3 cells by chemiluminescence assay	[PMID: 20403700]
NIH3T3	IC₅₀	0.3 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells without bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells without bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	16 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells Inhibition of PDGF-induced BrdU incorporation in 3T3 cells	[PMID: 12646019]
NIH3T3	IC₅₀	2 μM Compound: 5b	Inhibition of Vascular endothelial growth factor receptor in 3T3 cells Inhibition of Vascular endothelial growth factor receptor in 3T3 cells	[PMID: 12646019]
NIH3T3	IC₅₀	36 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 1% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 1% bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	49 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 5% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 5% bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	9.5 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin	[PMID: 12646019]
Sf9	IC₅₀	28.4 μM Compound: R2C3, 30	Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells	[PMID: 19674816]

In Vitro

SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (K_i=2.1 μM), FGFR1 trans-phosphorylation (K_i=1.2 μM), and PDGFR autophosphorylation (K_i=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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS No. 210644-62-5
Appearance Solid
Masse moléculaire 310.35
Formule C₁₈H₁₈N₂O₃
Color Orange to red
SMILES

O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C\2C=CC=C3)=O)=C1C.[(Z)]
Synonyms

(Z)-SU6668; (Z)-TSU-68
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (161.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

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

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Laird AD, et, al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60. [Content Brief]

[2]. Laird ad, et, al. SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. FASEB J. 2002 May;16(7):681-90. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2222 mL	16.1108 mL	32.2217 mL	80.5542 mL
	5 mM	0.6444 mL	3.2222 mL	6.4443 mL	16.1108 mL
	10 mM	0.3222 mL	1.6111 mL	3.2222 mL	8.0554 mL
	15 mM	0.2148 mL	1.0741 mL	2.1481 mL	5.3703 mL
	20 mM	0.1611 mL	0.8055 mL	1.6111 mL	4.0277 mL
	25 mM	0.1289 mL	0.6444 mL	1.2889 mL	3.2222 mL
	30 mM	0.1074 mL	0.5370 mL	1.0741 mL	2.6851 mL
	40 mM	0.0806 mL	0.4028 mL	0.8055 mL	2.0139 mL
	50 mM	0.0644 mL	0.3222 mL	0.6444 mL	1.6111 mL
	60 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3426 mL
	80 mM	0.0403 mL	0.2014 mL	0.4028 mL	1.0069 mL
	100 mM	0.0322 mL	0.1611 mL	0.3222 mL	0.8055 mL

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(Z)-Orantinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

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Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform PDGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

(Z)-Orantinib Related Classifications

HY-10517A Related Classifications