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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.

仅供研究使用。 我们不向患者出售。

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

订购信息

包装价格库存纯度备货期
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外观性状类白色固体
纯度98% Min.
存储 0-4℃,可保存几天到几周;-20℃,可保存 几个月。
可溶性溶于DMSO等有机溶剂
处理方式
运输条件可以在室温下进行运输。
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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