Cat. No.: HY-16018

Ilorasertib

(Synonyms: ABT-348)

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Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC₅₀s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

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Pureté: 99.86%
CAS No.: 1227939-82-3
Formule: C₂₅H₂₁FN₆O₂S
Masse moléculaire:488.54

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Ilorasertib Chemical Structure

CAS No.: 1227939-82-3

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Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- 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]

Aurora C

1 nM (IC₅₀)

Aurora B

7 nM (IC₅₀)

Aurora B (Y156H)

12 nM (IC₅₀)

Aurora A

120 nM (IC₅₀)

PDGFRα

11 nM (IC₅₀)

PDGFRβ

13 nM (IC₅₀)

VEGFR1

1 nM (IC₅₀)

VEGFR2

2 nM (IC₅₀)

VEGFR3

43 nM (IC₅₀)

FLT3

1 nM (IC₅₀)

CSF-1R

3 nM (IC₅₀)

c-KIT

20 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Aurora Kinase :

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform PDGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
NIH3T3	IC₅₀	3 nM Compound: 1 (ABT-348)	Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells	[PMID: 22695126]

In Vitro

Ilorasertib (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells^[2].
Ilorasertib (1-1000 nM) shows antiproliferative activity^[2].

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

Cell Viability Assay^[2]

Cell Line:

H1299, H460 cells
Concentration:

0, 3, 10, 30 nM
Incubation Time:

24 h
Result:

Induced a concentration-dependent increase in the extent and number of cells exhibiting polyploidy with EC₅₀S of 5, 10 nM for H1299, H460 cells, respectively.

Cell Proliferation Assay^[2]

Cell Line:

MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells
Concentration:

1-1000 nM
Incubation Time:
Result:

Showed antiproliferative activity with IC₅₀s of 0.3, 1, 103, 6, 6, 2, 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells, respectively.

In Vivo

Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in MV-4-11 tumor-bearing SCID mice with TGI of 80%, 86%, 94% at 6.25, 12.5, 25 mg/kg, respectively^[1].
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in SKM-1 tumor-bearing SCID mice with TGI of 38%, 59%, 80% at 6.25, 12.5, 25 mg/kg, respectively^[1].
Ilorasertib (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the histone H3 phosphorylation at 4-8 h in blood-borne tumor cells^[2].
Ilorasertib (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse^[2].
Ilorasertib (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse^[2].

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

Animal Model:

Female SCID/beige mice^[2]
Dosage:

25 mg/kg
Administration:

Subcutaneous minipump; 24 h
Result:

Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.

Animal Model:

22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))^[2]
Dosage:

20 mg/kg
Administration:

P.o.; once weekly for 3 weeks
Result:

Inhibited the tumor growth in mouse.

Essai clinique

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

Chemical Information

CAS No. 1227939-82-3
Appearance Solid
Masse moléculaire 488.54
Formule C₂₅H₂₁FN₆O₂S
Color Off-white to light yellow
SMILES

O=C(NC1=CC=CC(F)=C1)NC2=CC=C(C3=CSC4=C3C(N)=NC=C4C5=CN(CCO)N=C5)C=C2
Synonyms

ABT-348
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 41.67 mg/mL (85.29 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

2.0469 mL

10.2346 mL

20.4692 mL

5 mM

0.4094 mL

2.0469 mL

4.0938 mL

10 mM

0.2047 mL

1.0235 mL

2.0469 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. 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.26 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.26 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (281 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]. Yi-Chun Wang, et al. Abstract 858: Potent in vivo activity of the aurora kinase inhibitor ABT-348 in human acute myeloid leukemia and myelodysplastic syndrome xenograft models. Cancer Res (2012) 72 (8_Supplement): 858.

[2]. Glaser KB, et al. Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.0469 mL	10.2346 mL	20.4692 mL	51.1729 mL
	5 mM	0.4094 mL	2.0469 mL	4.0938 mL	10.2346 mL
	10 mM	0.2047 mL	1.0235 mL	2.0469 mL	5.1173 mL
	15 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4115 mL
	20 mM	0.1023 mL	0.5117 mL	1.0235 mL	2.5586 mL
	25 mM	0.0819 mL	0.4094 mL	0.8188 mL	2.0469 mL
	30 mM	0.0682 mL	0.3412 mL	0.6823 mL	1.7058 mL
	40 mM	0.0512 mL	0.2559 mL	0.5117 mL	1.2793 mL
	50 mM	0.0409 mL	0.2047 mL	0.4094 mL	1.0235 mL
	60 mM	0.0341 mL	0.1706 mL	0.3412 mL	0.8529 mL
	80 mM	0.0256 mL	0.1279 mL	0.2559 mL	0.6397 mL

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Ilorasertib

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Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform Aurora Kinase

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform PDGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ilorasertib Related Classifications

HY-16018 Related Classifications