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Purity: ≥98%
Ilorasertib (also known as ABT-348) is a potent, novel, orally bioavailable and ATP-competitive multi-kinase inhibitor with IC50s for inhibiting binding Aurora B (7 nM), C (1 nM), and A (120 nM), and also inhibits RET tyrosine kinase, PDGFRβ, and Flt1 with IC50s of 7 nM, 3 nM and 32 nM. ABT 348 was assessed and found to be efficacious in representative solid tumor (HT1080 and MiaPaCa, tumor stasis) and hematological malignancy (RS4;11, regression) xenografts due to its distinct spectrum of activity. The rationale behind evaluating ABT-348 clinically as a therapeutic agent for cancer treatment is provided by these findings.
| Targets |
Aurora C (IC50 = 1 nM); Aurora B (IC50 = 7 nM); Aurora B (Y156H) (IC50 = 12 nM); Aurora A (IC50 = 120 nM); PDGFRα (IC50 = 11 nM); PDGFRβ (IC50 = 13 nM); VEGFR1 (IC50 = 1 nM); VEGFR2 (IC50 = 2 nM); VEGFR3 (IC50 = 43 nM); FLT3 (IC50 = 1 nM); CSF-1R (IC50 = 3 nM); c-KIT (IC50 = 20 nM)
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| ln Vitro |
Ilorasertib (0, 3, 10, 30 nM; 24 h) causes an increase in H1299, H460 cell extent and number that is concentration-dependent[2].
Ilorasertib (1-1000 nM) demonstrates antiproliferative properties [2]. |
| ln Vivo |
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) demonstrates anti-tumor activity in SCID mice bearing MV-4-11 tumors, with TGI values of 80%, 86%, and 94% at 6.25, 12.5, and 25 mg/kg, respectively[1].
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) demonstrates antitumor activity in SCID mice bearing SKM-1 tumors, with TGI values of 38%, 59%, and 80% at 6.25, 12.5, and 25 mg/kg, respectively[1]. Ilorasertib (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the phosphorylation of histone H3 in blood-borne tumor cells between 4 and 8 hours[2]. Ilorasertib (0.2 mg/kg; i.v.) exhibits anti-VEGF activity in mice[2]. Ilorasertib (20 mg/kg; p.o.;once weekly for 3 weeks) exhibits antitumor activity in mouse[2]. |
| Cell Assay |
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. |
| Animal Protocol |
Female SCID/beige mice[2]
25 mg/kg Subcutaneous minipump; 24 h |
| References |
|
| Molecular Formula |
C25H21N6O2FS
|
|---|---|
| Molecular Weight |
488.537
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| Exact Mass |
488.14
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| Elemental Analysis |
C, 61.46; H, 4.33; F, 3.89; N, 17.20; O, 6.55; S, 6.56
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| CAS # |
1227939-82-3
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| Related CAS # |
Ilorasertib hydrochloride;1847485-91-9
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=CC(=C1)F)NC(=O)NC2=CC=C(C=C2)C3=CSC4=C3C(=NC=C4C5=CN(N=C5)CCO)N
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| InChi Key |
WPHKIQPVPYJNAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H21FN6O2S/c26-17-2-1-3-19(10-17)31-25(34)30-18-6-4-15(5-7-18)21-14-35-23-20(12-28-24(27)22(21)23)16-11-29-32(13-16)8-9-33/h1-7,10-14,33H,8-9H2,(H2,27,28)(H2,30,31,34)
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| Chemical Name |
1-[4-[4-amino-7-[1-(2-hydroxyethyl)pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl]phenyl]-3-(3-fluorophenyl)urea
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| Synonyms |
Abbott-968660; Ilorasertib; ABT348; ABT-348; ABT 348; Abbott 968660
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~41.7 mg/mL (~85.3 mM)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02540876 | Completed | Other: Laboratory Biomarker Analysis Drug: Ilorasertib |
Metastatic Malignant Neoplasm Solid Neoplasm |
University of Chicago | September 8, 2015 | Phase 1 |
| NCT01110473 | Completed | Drug: ABT-348 and azacitidine Drug: ABT-348 |
Myelodysplasia Chronic Myelogenous Leukemia |
AbbVie (prior sponsor, Abbott) |
April 2010 | Phase 1 |
| NCT01110486 | Recruiting | Drug: ABT-348 Drug: ABT-348 and carboplatin |
Advanced Solid Tumors | AbbVie (prior sponsor, Abbott) |
March 2010 | Phase 1 |
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