2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK
  3. Aurora Kinase VEGFR PDGFR
  4. Ilorasertib

Ilorasertib  (Synonyms: ABT-348)

Cat. No.: HY-16018 Purity: 99.86%
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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).

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

Ilorasertib Chemical Structure

Ilorasertib Chemical Structure

CAS No. : 1227939-82-3

Size Price Stock Quantity
5 mg USD 140 In-stock
10 mg USD 235 In-stock
25 mg USD 490 In-stock
50 mg USD 780 In-stock
100 mg USD 1200 In-stock
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Other Forms of Ilorasertib:

Ilorasertib Related Antibodies

Top Publications Citing Use of Products

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Aurora Kinase Aurora A Aurora B Aurora C

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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)[1][2].

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)

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.

Ilorasertib Related Antibodies

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.
Clinical Trial
Molecular Weight

488.54

Formula

C25H21FN6O2S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0469 mL 10.2346 mL 20.4692 mL
5 mM 0.4094 mL 2.0469 mL 4.0938 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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).
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.
Purity & Documentation
References

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. 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 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:

Ilorasertib1227939-82-3ABT-348ABT348ABT 348Aurora KinaseVEGFRPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptorantiproliferative activityH1299H460 cellsanti-tumorhistone H3 phosphorylationAMLMDSInhibitorinhibitorinhibit

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