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Ifebemtinib

Catalog No: 24092
CAS Number: 1227948-82-4
Purity: 98% Min.

 Ifebemtinib, also known as BI-853520 and IN-10018, is a novel, highly selective PTK2 kinase inhibitor that demonstrates anti-tumor activity in vitro and in vivo. BI 853520 inhibits spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. BI 853520 inhibited spheroid growth and significantly reduced tumor weight, cell proliferation, and MVD in vivo. In vitro, the compound inhibits FAK autophosphorylation in PC-3 prostate carcinoma cells with an IC50 of 1 nmol/L and blocks anchorage-independent proliferation of PC-3 cells with an EC50 of 3 nmol/L, whereas cells grown in conventional surface culture are 1000-fold less sensitive.

For research use only. We do not sell to patients.

Chemical Information

NameIfebemtinib
Iupac Chemical Name4-[[4-[(2,3-Dihydro-2-methyl-3-oxo-1H-isoindol-4-yl)oxy]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)benzamide
SynonymsBI853520; BI 853520; BI-853520; IN-10018; IN10018; IN 10018; Ifebemtinib;
Molecular FormulaC28H28F4N6O4
Molecular Weight588.55
SmileO=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(C(F)(F)F)C(OC4=CC=CC(CN5C)=C4C5=O)=N3)C=C2F
InChiKeyULMMVBPTWVRPSI-UHFFFAOYSA-N
InChiInChI=1S/C28H28F4N6O4/c1-37-9-7-16(8-10-37)34-24(39)17-11-22(41-3)20(12-19(17)29)35-27-33-13-18(28(30,31)32)25(36-27)42-21-6-4-5-15-14-38(2)26(40)23(15)21/h4-6,11-13,16H,7-10,14H2,1-3H3,(H,34,39)(H,33,35,36)
CAS Number1227948-82-4
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Ordering Information

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FormulationOff-white solid
Purity98% Min.
StorageDry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
SolubilitySoluble in DMSO
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Pang XJ, Liu XJ, Liu Y, Liu WB, Li YR, Yu GX, Tian XY, Zhang YB, Song J, Jin CY, Zhang SY. Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy. Molecules. 2021 Jul 13;26(14):4250. doi: 10.3390/molecules26144250. PMID: 34299525; PMCID: PMC8308130.


2: Mohanty A, Pharaon RR, Nam A, Salgia S, Kulkarni P, Massarelli E. FAK- targeted and combination therapies for the treatment of cancer: an overview of phase I and II clinical trials. Expert Opin Investig Drugs. 2020 Apr;29(4):399-409. doi: 10.1080/13543784.2020.1740680. Epub 2020 Mar 19. PMID: 32178538.


3: Lee RC, Gan HK. BI 853520, a FAK-Simile of Prior FAK Inhibitors? Target Oncol. 2019 Feb;14(1):39-41. doi: 10.1007/s11523-019-00621-z. PMID: 30843167.


4: de Jonge MJA, Steeghs N, Lolkema MP, Hotte SJ, Hirte HW, van der Biessen DAJ, Abdul Razak AR, De Vos FYFL, Verheijen RB, Schnell D, Pronk LC, Jansen M, Siu LL. Phase I Study of BI 853520, an Inhibitor of Focal Adhesion Kinase, in Patients with Advanced or Metastatic Nonhematologic Malignancies. Target Oncol. 2019 Feb;14(1):43-55. doi: 10.1007/s11523-018-00617-1. PMID: 30756308; PMCID: PMC6407740.


5: Verheijen RB, van der Biessen DAJ, Hotte SJ, Siu LL, Spreafico A, de Jonge MJA, Pronk LC, De Vos FYFL, Schnell D, Hirte HW, Steeghs N, Lolkema MP. Randomized, Open-Label, Crossover Studies Evaluating the Effect of Food and Liquid Formulation on the Pharmacokinetics of the Novel Focal Adhesion Kinase (FAK) Inhibitor BI 853520. Target Oncol. 2019 Feb;14(1):67-74. doi: 10.1007/s11523-018-00618-0. PMID: 30742245; PMCID: PMC6407750.


6: Doi T, Yang JC, Shitara K, Naito Y, Cheng AL, Sarashina A, Pronk LC, Takeuchi Y, Lin CC. Phase I Study of the Focal Adhesion Kinase Inhibitor BI 853520 in Japanese and Taiwanese Patients with Advanced or Metastatic Solid Tumors. Target Oncol. 2019 Feb;14(1):57-65. doi: 10.1007/s11523-019-00620-0. PMID: 30725402; PMCID: PMC6407737.


7: Laszlo V, Valko Z, Ozsvar J, Kovacs I, Garay T, Hoda MA, Klikovits T, Stockhammer P, Aigner C, Gröger M, Klepetko W, Berger W, Grusch M, Tovari J, Waizenegger IC, Dome B, Hegedus B. The FAK inhibitor BI 853520 inhibits spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. J Mol Med (Berl). 2019 Feb;97(2):231-242. doi: 10.1007/s00109-018-1725-7. Epub 2018 Dec 11. PMID: 30539198; PMCID: PMC6348072.


8: Tiede S, Meyer-Schaller N, Kalathur RKR, Ivanek R, Fagiani E, Schmassmann P, Stillhard P, Häfliger S, Kraut N, Schweifer N, Waizenegger IC, Bill R, Christofori G. The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer. Oncogenesis. 2018 Sep 20;7(9):73. doi: 10.1038/s41389-018-0083-1. PMID: 30237500; PMCID: PMC6148276.


9: Hirt UA, Waizenegger IC, Schweifer N, Haslinger C, Gerlach D, Braunger J, Weyer-Czernilofsky U, Stadtmüller H, Sapountzis I, Bader G, Zoephel A, Bister B, Baum A, Quant J, Kraut N, Garin-Chesa P, Adolf GR. Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype. Oncogenesis. 2018 Feb 23;7(2):21. doi: 10.1038/s41389-018-0032-z. PMID: 29472531; PMCID: PMC5833389.

Chemical Structure

24092 - Ifebemtinib | CAS 1227948-82-4

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