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  3. Chiauranib

Chiauranib  (Synonyms: Ibcasertib; CS2164)

Cat. No.: HY-124526 Purity: 99.28%
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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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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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.

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.
Clinical Trial
Molecular Weight

435.47

Formula

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

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 available by MedChemExpress (MCE).
Purity & Documentation
References
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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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Product Name:
Chiauranib
Cat. No.:
HY-124526
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