Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H21FN6O2S |
Molecular Weight | 488.537 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC=C(C2=CN(CCO)N=C2)C3=C1C(=CS3)C4=CC=C(NC(=O)NC5=CC(F)=CC=C5)C=C4
InChI
InChIKey=WPHKIQPVPYJNAX-UHFFFAOYSA-N
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)
Molecular Formula | C25H21FN6O2S |
Molecular Weight | 488.537 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Ilorasertib (previously known as ABT-348), an orally bioavailable ATP-competitive inhibitor of Aurora kinases (A, B and C), as well as the VEGF and PDGF families of receptor tyrosine kinases, was developed by AbbVie as an antineoplastic agent. It is known that Aurora kinases A, B, and C play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types. Both VEGFRs and PDGFRs may be upregulated in various tumor cell types. 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. Ilorasertib participated in phase I clinical for patients with advanced hematologic malignancies. The result has shown that the drug could be further studied in acute myelogenous leukemia. Ilorasertib is also going to be studied in phase II clinical trials to learn if this drug can help to control CDKN2A-deficient cancer in patients with advanced cancers.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02478320
Part 1 Dose of Ilorasertib: 200 mg administered by mouth twice daily on Days 1, 8, and 15 of each 28-day cycle. Part 2 Expansion: Ilorasertib200 mg administered by mouth twice daily on Days 1, 8, and 15 of each 28-day cycle.
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 01:29:28 GMT 2023
by
admin
on
Sat Dec 16 01:29:28 GMT 2023
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Record UNII |
6L5D03D975
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
364212
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FDA ORPHAN DRUG |
337811
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NCI_THESAURUS |
C1404
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NCI_THESAURUS |
C129825
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DTXSID10153718
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46207586
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CHEMBL1980297
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6L5D03D975
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YY-111
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1227939-82-3
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DB11694
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100000175009
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EU/3/12/1001(WITHDRAWN)
Created by
admin on Sat Dec 16 01:29:28 GMT 2023 , Edited by admin on Sat Dec 16 01:29:28 GMT 2023
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PRIMARY | Please note that this product was withdrawn from the Community Register of designated Orphan Medicinal Products in April 2015 on request of the Sponsor. On 6 June 2012, orphan designation (EU/3/12/1001) was granted by the European Commission to Abbott Laboratories, United Kingdom, for 1-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl] thieno [3,2-c]pyridin-3-yl}phenyl)-3-(3-fluorophenyl)urea for the treatment of ovarian cancer. The sponsorship was transferred to AbbVie Ltd, United Kingdom, in January 2013. | ||
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EU/3/11/915(WITHDRAWN)
Created by
admin on Sat Dec 16 01:29:28 GMT 2023 , Edited by admin on Sat Dec 16 01:29:28 GMT 2023
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PRIMARY | Please note that this product was withdrawn from the Community Register of designated Orphan Medicinal Products in April 2015 on request of the Sponsor. On 27 October 2011, orphan designation (EU/3/11/915) was granted by the European Commission to Abbott Laboratories, United Kingdom, for 1-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H- pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-3-(3-fluorophenyl)urea for the treatment of acute myeloid leukaemia. The sponsorship was transferred to AbbVie Ltd, United Kingdom, in January 2013. | ||
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C116729
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9670
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