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Ifebemtinib

编号: 24092
Cas号: 1227948-82-4
纯度: 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.

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化学信息

名称Ifebemtinib
Iupac 化学名称4-[[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
同义词BI853520; BI 853520; BI-853520; IN-10018; IN10018; IN 10018; Ifebemtinib;
英文同义词BI853520; BI 853520; BI-853520; IN-10018; IN10018; IN 10018; Ifebemtinib;
分子式C28H28F4N6O4
分子量588.55
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号1227948-82-4
相关CAS号

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外观性状Off-white solid
纯度98% Min.
存储Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
可溶性Soluble in DMSO
处理方式
运输条件Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
海关编码
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.

化学结构

24092 - Ifebemtinib | CAS 1227948-82-4

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