1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor VEGFR c-Met/HGFR
  3. Ningetinib

Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

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

Ningetinib Chemical Structure

Ningetinib Chemical Structure

CAS No. : 1394820-69-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

IC50 & Target[1]

VEGFR2

1.9 nM (IC50)

In Vitro

Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively[1].

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

In Vivo

When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%, p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group[1].

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

Clinical Trial
Molecular Weight

556.58

Formula

C31H29FN4O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C(NC2=CC(F)=C(OC3=CC=NC4=C3C=CC(OCC(C)(O)C)=C4)C=C2)=O)C(N(C5=CC=CC=C5)N1C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (22.46 mM; ultrasonic and warming and heat to 60°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 1.7967 mL 8.9834 mL 17.9669 mL
5 mM 0.3593 mL 1.7967 mL 3.5934 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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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 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.
Calculation results:
Working solution concentration: mg/mL
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7967 mL 8.9834 mL 17.9669 mL 44.9172 mL
5 mM 0.3593 mL 1.7967 mL 3.5934 mL 8.9834 mL
10 mM 0.1797 mL 0.8983 mL 1.7967 mL 4.4917 mL
15 mM 0.1198 mL 0.5989 mL 1.1978 mL 2.9945 mL
20 mM 0.0898 mL 0.4492 mL 0.8983 mL 2.2459 mL
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Ningetinib 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.

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Ningetinib
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