2. Protein Tyrosine Kinase/RTK
  3. VEGFR PDGFR
  4. Ansornitinib

Ansornitinib  (Synonyms: ANG-3070)

Cat. No.: HY-147243 Purity: 98.04%
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Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.

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

Ansornitinib Chemical Structure

Ansornitinib Chemical Structure

CAS No. : 1448874-96-1

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5 mg USD 385 In-stock
10 mg USD 616 In-stock
25 mg USD 1294 In-stock
50 mg USD 2070 In-stock
100 mg USD 3313 In-stock
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Based on 1 publication(s) in Google Scholar

Ansornitinib Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases[1].

In Vitro

Ansornitinib (compound I) (0.1 nM-10 μM, 2 h) can significantly inhibit the phosphorylation of PDGFRβ in human hepatic stellate cells and KDR phosphorylation in human umbilical vein endothelial cells (HUVEC)[1].
Ansornitinib (compound I) (0.1-13 μM, 48 h) can induce a decrease in the expression of many different inflammation-related markers, such as macrophage colony-stimulating factor (M-CSF), soluble interleukin 8, and fibrosis-related markers, such as N-calmodulin, α-SMA, etc., in a dose-dependent manner[1].

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

Ansornitinib Related Antibodies
In Vivo

Ansornitinib (compound I) (25 mg/kg, p.o., twice a day, 4 weeks) can reduce fibrosis in TGFβ positive female mice[1].
Ansornitinib (compound I) (5-45 mg/kg, p.o., twice a day, 4 days) can reduce inflammatory bowel disease (IBD) in TNBS-induced IBD/acute colitis male CD-1 mice[1].

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

Animal Model: 8-10 weeks TGFβ positive female mice[1]
Dosage: 25 mg/kg
Administration: Oral administration; twice a day; 4 weeks
Result: Reduced lung fibrosis score, lung hydroxyproline levels and αSMA, a marker of early pulmonary fibrosis.
Animal Model: TNBS-induced IBD/acute colitis male CD-1 mice[1]
Dosage: 5, 15, 45 mg/kg
Administration: Oral administration; twice a day; 4 days
Result: Improved colonic histology and reduced the TNBS-induced loss of cupped cells at 15 mg/kg and 45 mg/kg significantly.
Reduced the expression level of myeloperoxidase (MPO) at 5 mg/kg and 15 mg/kg significantly while there was no statistical difference at 45 mg/kg.
Animal Model: Male Sprague Dawley rats[1]
Dosage: 30 mg/kg
Administration: Intravenous injection; once
Result: The pharmacokinetic parameters of Ansornitinib (compound I)
Parameter Ansornitinib (compound I)
t1/2 4.1 h
Tmax 0.518 h
Cmax 7860 ng/mL
Clearance 173 mL/kg/min
steady-state volume 18.2 L/kg
AUC0-last 3180 ng/mL*h
AUC0‑inf_obs 3200 ng/mL*h
Molecular Weight

540.61

Formula

C30H32N6O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN(CC1)CCN1CC(N(C)C(C=C2)=CC=C2N/C(C3=CC=CC=C3)=C4C5=CC=C(C(OC)=O)N=C5NC/4=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 : 40 mg/mL (73.99 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8498 mL 9.2488 mL 18.4976 mL
5 mM 0.3700 mL 1.8498 mL 3.6995 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: 5 mg/mL (9.25 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 5 mg/mL (9.25 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8498 mL 9.2488 mL 18.4976 mL 46.2441 mL
5 mM 0.3700 mL 1.8498 mL 3.6995 mL 9.2488 mL
10 mM 0.1850 mL 0.9249 mL 1.8498 mL 4.6244 mL
15 mM 0.1233 mL 0.6166 mL 1.2332 mL 3.0829 mL
20 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
25 mM 0.0740 mL 0.3700 mL 0.7399 mL 1.8498 mL
30 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5415 mL
40 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
50 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9249 mL
60 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
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Ansornitinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ansornitinib1448874-96-1ANG-3070ANG3070ANG 3070VEGFRPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptoransornitinibantifibrotic agentfibrotic diseaseskinase inhibitorVEGFR2Inhibitorinhibitorinhibit

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