A multi-kinase inhibitor
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Ilorasertib

Item No. 34204

Technical Information
Formal Name
N-[4-[4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl]phenyl]-N′-(3-fluorophenyl)-urea
CAS Number
1227939-82-3
Synonyms
  • ABT-348
Molecular Formula
C25H21FN6O2S
Formula Weight
Purity
≥98%
A solid
Ethanol: soluble
λmax
261 nm
SMILES
O=C(NC1=CC(F)=CC=C1)NC2=CC=C(C3=CSC4=C(C5=CN(CCO)N=C5)C=NC(N)=C43)C=C2
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)
InChi Key
WPHKIQPVPYJNAX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Ilorasertib is a multi-kinase inhibitor.1 It inhibits Aurora C, VEGFR1, VEGFR2, FLT3, colony-stimulating factor 1 receptor (CSF1R), and Aurora B (IC50s = 1, 1, 2, 1, 3, and 7 nM, respectively). It also inhibits PDGFRα, PDGFRβ, c-Kit, VEGFR3, and Aurora A (IC50s = 11, 13, 20, 43, and 120 nM, respectively). Ilorasertib inhibits autophosphorylation of Aurora A, -B, and -C in HeLa cells with IC50 values of 189, 13, and 13 nM, respectively. It inhibits proliferation of a variety of cancer cells, including MV4-11 acute myeloid leukemia (AML), SUP-B15 acute lymphocytic leukemia (ALL), and H1299 non-small cell lung cancer (NSCLC) cells (IC50s = 0.3, 4, and 2 nM, respectively). It decreases histone H3 phosphorylation in blood-borne tumor cells in an engrafted mouse model of leukemia when administered at a dose of 25 mg/kg and reduces tumor growth in fibrosarcoma, pancreatic carcinoma, ALL, and multiple myeloma mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Glaser, K.B., Li, J., Marcotte, P.A., et alPreclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J. Pharmacol. Exp. Ther. 343(3), 617-627 (2012).