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
COA Handling Instructions

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).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Ilorasertib hydrochloride) usually boasts enhanced water solubility and stability.

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

Ilorasertib Chemical Structure

Ilorasertib Chemical Structure

CAS No. : 1227939-82-3

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50 mg USD 600 Ask For Quote & Lead Time
100 mg USD 1100 Ask For Quote & Lead Time

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Other In-stock Forms of Ilorasertib:

Other Forms of Ilorasertib:

Ilorasertib Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
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

  • Customer Review

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].

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].

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

Appearance

Solid

Formula

C25H21FN6O2S
CAS No.
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)

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
10 mM 0.2047 mL 1.0235 mL 2.0469 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

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