2. Protein Tyrosine Kinase/RTK Epigenetics Cell Cycle/DNA Damage
  3. Mitosis VEGFR Aurora Kinase c-Kit c-Fms PDGFR
  4. Chiauranib

Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.

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Chiauranib

Chiauranib Chemical Structure

CAS No. : 1256349-48-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
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Chiauranib Related Antibodies

Top Publications Citing Use of Products

Voir tous les produits spécifiques à Isoform VEGFR:

Voir toutes les isoformes
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Voir tous les produits spécifiques à Isoform Aurora Kinase:

Voir toutes les isoformes
Aurora Kinase Aurora A Aurora B Aurora C

Voir tous les produits spécifiques à Isoform PDGFR:

Voir toutes les isoformes
PDGFR PDGFRβ PDGFRα

  • Activité biologique

  • Pureté et documentation

  • Références

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Description

Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects[1].

IC50 & Target[1]

Flt-1

8 nM (IC50)

KDR

7 nM (IC50)

Flt-4

9 nM (IC50)

PDGFRα

1 nM (IC50)

c-Kit

4 nM (IC50)

Aurora B

9 nM (IC50)

PDGFRβ

93 nM (IC50)

CSF-1R

7 nM (IC50)

In Vitro

Chiauranib (CS2164; 3 μM; 24 hours) shows induction of G2/M cell cycle arrest and suppression of cell proliferation in tumor tissues through the inhibition of Aurora B-mediated H3 phosphorylation[1].
In HUVEC and PDGFRβ phosphorylation in PDGFRβ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) displays anti-angiogenic activities through suppression of VEGFR/PDGFR phosphorylation, inhibition of ligand-dependent cell proliferation and capillary tube formation, and prevention of vasculature formation in tumor tissues[1].
. Chiauranib (CS2164) inhibits CSF-1R phosphorylation that leads to the suppression of ligand-stimulated monocyte-to-macrophage differentiation and reduces CSF-1R+ cells in tumor tissues[1].

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

Chiauranib Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Molt-4 cells
Concentration: 3 μM
Incubation Time: 24 hours
Result: Induced the pronounced cell cycle arrest in the G2/M phase at 3 μM.

Western Blot Analysis[1]

Cell Line: Molt-4 cells
Concentration: 1.5 μM, 3 μM, 6 μM
Incubation Time: 24 hours
Result: Yielded a substantial reduction in the level of p-H3 in Molt‐4 cells in a concentration-dependent fashion.
In Vivo

Chiauranib (CS2164; 0.5-40 mg/kg; oral administration; once daily; for 33 days or 43 days) treatment induces remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models. Chiauranib exhibits broad and potent in vivo anti-tumor activities[1].

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

Animal Model: Female BALB/c athymic (nu+/nu+) mice (6-week old) bearing HCT-8, SMMC-7721, MGC‐803 or A549 cells[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg
Administration: Oral administration; once daily; for 33 days or 43 days
Result: Induced remarkable regression or complete inhibition of tumor growth in several human tumor xenograft models.
Essai clinique
Masse moléculaire

435.47

Formule

C27H21N3O3
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

O=C(NC1=CC=CC=C1N)C2=C3C=CC(OC4=CC=NC5=CC(OC)=CC=C54)=CC3=CC=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité
In Vitro: 

DMSO : 62.5 mg/mL (143.52 mM; Need ultrasonic; 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 2.2964 mL 11.4818 mL 22.9637 mL
5 mM 0.4593 mL 2.2964 mL 4.5927 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 (protect from light). 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

  • Calculateur de dilution

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    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.

    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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.
Pureté et documentation

Purity: 98.97%

SDS (393 KB)

COA (254 KB) LCMS (103 KB)

Instruction de manipulation (2659 KB)
Références

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 (protect from light). 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 2.2964 mL 11.4818 mL 22.9637 mL 57.4092 mL
5 mM 0.4593 mL 2.2964 mL 4.5927 mL 11.4818 mL
10 mM 0.2296 mL 1.1482 mL 2.2964 mL 5.7409 mL
15 mM 0.1531 mL 0.7655 mL 1.5309 mL 3.8273 mL
20 mM 0.1148 mL 0.5741 mL 1.1482 mL 2.8705 mL
25 mM 0.0919 mL 0.4593 mL 0.9185 mL 2.2964 mL
30 mM 0.0765 mL 0.3827 mL 0.7655 mL 1.9136 mL
40 mM 0.0574 mL 0.2870 mL 0.5741 mL 1.4352 mL
50 mM 0.0459 mL 0.2296 mL 0.4593 mL 1.1482 mL
60 mM 0.0383 mL 0.1914 mL 0.3827 mL 0.9568 mL
80 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7176 mL
100 mM 0.0230 mL 0.1148 mL 0.2296 mL 0.5741 mL
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Chiauranib 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:

Chiauranib1256349-48-0Ibcasertib CS2164CS2164CS 2164CS-2164MitosisVEGFRAurora Kinasec-Kitc-FmsPDGFRVascular endothelial growth factor receptorSCFRCD117CSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RPlatelet-derived growth factor receptoranti-angiogenesisVEGFR1VEGFR2VEGFR3PDGFRαAurora-BanticancerInhibitorinhibitorinhibit

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