Initial in vivo testing of a multitarget kinase inhibitor, regorafenib, by the Pediatric Preclinical Testing Consortium.

Initial in vivo testing of a multitarget kinase inhibitor, regorafenib, by the Pediatric Preclinical Testing Consortium.
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DOI:
10.1002/pbc.28222
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发表时间:
2020-06
影响因子:
3.2
通讯作者:
Gorlick R
Gorlick R
中科院分区:
医学3区
文献类型:
--
作者:
Harrison DJ;Gill JD;Roth ME;Zhang W;Teicher B;Erickson S;Gatto G;Kurmasheva RT;Houghton PJ;Smith MA;Kolb EA;Gorlick R

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Regorafenib是一种小分子多激酶抑制剂,可抑制多种激酶,包括BRAF、KIT、PDGFRb、RAF、RET和VEGFR1-3。在6个骨肉瘤模型、3个横纹肌肉瘤模型和1个尤文肉瘤模型中,Regorafenib的体内抗癌作用被评估。在评价瑞格非尼诱导的适度抑制肿瘤生长的模型中。对瑞格拉非尼的总体反应模式似乎类似于激酶抑制剂索拉非尼,在某些模型中,肿瘤生长明显放缓,仅限于给药时间,这是主要的治疗效果。
Regorafenib is a small molecule multikinase inhibitor that inhibits multiple kinases including BRAF, KIT, PDGFRB, RAF, RET, and VEGFR1–3. The in vivo anticancer effects of regorafenib were assessed in a panel of six osteosarcoma models, three rhabdomyosarcoma models, and one Ewing sarcoma model. Regorafenib induced modest inhibition of tumor growth in the models evaluated. The overall pattern of response to regorafenib appears similar to that of the kinase inhibitor sorafenib, with pronounced slowing of tumor growth in some models, limited to the period of agent administration, being the primary treatment effect.
DOI: 10.1371/journal.pone.0142612
发表时间: 2015
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