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

Chiauranib (Synonyms: CS2164)

Cat. No.: HY-124526 Purity: 99.28%
Handling Instructions

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.

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

Chiauranib Chemical Structure

Chiauranib Chemical Structure

CAS No. : 1256349-48-0

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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].

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

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].

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.
Clinical Trial
Molecular Weight

435.47

Formula

C₂₇H₂₁N₃O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (143.52 mM; Need ultrasonic)

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
10 mM 0.2296 mL 1.1482 mL 2.2964 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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