Cat. No.: HY-124526

Chiauranib

(Synonyms: Ibcasertib; CS2164)

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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.

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Pureté: 98.97%
CAS No.: 1256349-48-0
Formule: C₂₇H₂₁N₃O₃
Masse moléculaire:435.47

Stockage:

4°C, protect from light

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

Chiauranib Chemical Structure

CAS No.: 1256349-48-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)

Voir tous les produits spécifiques à Isoform PDGFR :

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform Aurora Kinase :

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1256349-48-0
Appearance Solid
Masse moléculaire 435.47
Formule C₂₇H₂₁N₃O₃
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
Synonyms

Ibcasertib; CS2164
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. You Zhou, et al. CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci. 2017 Mar;108(3):469-477. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Voir tous les produits spécifiques à Isoform PDGFR

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform Aurora Kinase

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Chiauranib Related Classifications

HY-124526 Related Classifications