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

Ilorasertib (Synonyms: ABT-348)

Cat. No.: HY-16018
Handling Instructions

Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.

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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Description

Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.

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 is an ATP-competitive multitargeted kinase inhibitor with IC50 for inhibiting cellular autophosphorylation of Aurora B (13 nM), C (13 nM), and A (189 nM). In addition to targeting Aurora kinases, Ilorasertib is a potent inhibitor of the VEGFR and PDGFR kinase families and, to a lesser extent, the Src family of cytoplasmic tyrosine kinases. Ilorasertib induces a concentration-dependent increase in the extent and number of two NSCLC cell lines exhibiting polyploidy. The potency for inducing this response (EC50 = 5 and 10 nM). Ilorasertib shows antiproliferative activity against BCR-ABL expressing CML cells and cells expressing the gleevec-resistant BCR-ABL T315I mutation (IC50 = 47 and 260 nM)[2].

In Vivo

Ilorasertib (25 mg/kg, s.c.) leads to an inhibition of histone H3 phosphorylation in circulating tumor cells obtained from an engrafted leukemia model. Ilorasertib inhibits the VEGF response with a potency (ED50 = 0.2 mg/kg i.v.) in a uterine edema model. Ilorasertib (20 mg/kg, p.o.) inhibits the growth of established tumors and causes regression of advanced tumors in human xenograft models[2]. Ilorasertib demonstrates significant antitumor efficacy in both solid and hematological xenograft models after intravenous, mini-pump or parenteral once-weekly dosing[3].

Clinical Trial
Molecular Weight

488.54

Formula

C₂₅H₂₁FN₆O₂S

CAS No.

1227939-82-3

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (85.29 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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 provided by MCE.
References
Cell Assay
[2]

Carcinoma cells (2500 cells/well) are plated overnight in full-growth medium (containing 10% FBS). Compound is added to the cells in full-growth medium and incubated for 72 h at 37°C in a CO2 incubator. For leukemia cells, generally 50,000 cells/well are plated in full-growth medium, drug is added, and they are incubated for 72 h. The effects on proliferation are determined by the addition of alamarBlue (final solution 10%), incubation for 4 h, and analysis in a fluorescence plate reader (excitation 544; emission 590), or alternatively, medium is removed and replaced with 200 μL of Cell TiterGlo reagent and analyzed for luminescence. Noncycling primary HUVEC are used to assess the effect of Ilorasertib on nonproliferating cells. Cells (35,000/well) are seeded in growth medium in a 96-well tissue culture plate, and after 2 days, the medium is changed and the cells are treated with Ilorasertib. After an additional 3 days, cell viability is measured with Cell TiterGlo reagent.

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

Animal Administration

sup>[2]For flank xenograft models, cells are suspended in PBS, mixed with Matrigel (phenol red free) in a ratio of 1:4 (v/v), and inoculated into the flank of female SCID/beige mice (5 million cells per site). Inoculated mice are randomized into groups of 10, and treatment is initiated when mean tumor volume is approximately 0.4 cm3 or 0.5 cm3. Tumor growth in the flank is assessed by measuring tumor size with calipers and calculating volume using the formula (L × W2/2). Study groups are terminated before tumor volume reaches 3 cm3. Inhibition of tumor growth is assessed at the time the vehicle-treated group is terminated by calculating the ratio of the mean volume of the test drug group to the mean volume of the untreated (control) group (T/C) and calculating the percentage of inhibition of control [(1 − T/C) × 100]. The dosing formulation of test agents is prepared by stepwise addition, with mixing, of the following reagents: EtOH, Tween 80, polyethylene glycol 400, and 2% hydroxypropyl methylcellulose (2:5:20:73, v/v). Dosing volume is 10 mL/kg.

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

References
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Ilorasertib
Cat. No.:
HY-16018
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