Ilorasertib - CAS 1227939-82-3
Catalog number:
1227939-82-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Description:
Ilorasertib, also know as ABT-348, is a novel, potent and orally bioavailable inhibitor of the Aurora kinases as well as the VEGF and PDGF families of receptor tyrosine kinases and is currently in Phase I clinical trials. ABT-348 has nanomolar potency (IC50) for inhibiting binding and cellular auto-phosphorylation of Aurora B (7 and 13 nM), C (1 and 13 nM) and A (120 and 189 nM). These results provide the rationale for clinical assessment of ABT-348 as a therapeutic agent in the treatment of cancer.
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Purity:
0.98
Appearance:
Solid powder
Synonyms:
ABT-348; Abbott 968660.
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Current Developer:
Abbott Laboratories, Inc.
1.Phase 1 dose escalation trial of ilorasertib, a dual Aurora/VEGF receptor kinase inhibitor, in patients with hematologic malignancies.
Garcia-Manero G1, Tibes R, Kadia T, Kantarjian H, Arellano M, Knight EA, Xiong H, Qin Q, Munasinghe W, Roberts-Rapp L, Ansell P, Albert DH, Oliver B, McKee MD, Ricker JL, Khoury HJ. Invest New Drugs. 2015 Aug;33(4):870-80. doi: 10.1007/s10637-015-0242-6. Epub 2015 May 2.
BACKGROUND: Ilorasertib (ABT-348) is a novel inhibitor of Aurora kinase, vascular endothelial growth factor (VEGF) and platelet-derived growth factor receptors, and the Src families of tyrosine kinases. Ilorasertib alone or in combination with azacitidine demonstrated activity in preclinical models in various hematological malignancies, indicating that pan-Aurora kinase and multiple kinase inhibition may have preferential antileukemic activity. This phase 1 trial determined the safety, pharmacokinetics, and preliminary antitumor activity of ilorasertib alone or combined with azacitidine in advanced hematologic malignancies.
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CAS 1227939-82-3 Ilorasertib

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