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BI-847325

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BI-847325ÊÇÒ»ÖÖ¿Ú·þ¾ßÓÐÉúÎï»îÐÔµÄÑ¡ÔñÐÔµÄË«ÖØMEK/Aurora kinaseÒÖÖƼÁ£¬¶Ô·ÇÖÞצó¸Aurora B£¬ÈËAurora A ºÍAurora C£¬ÒÔ¼°ÈËMEK1 ºÍMEK2µÄIC50·Ö±ðΪ3 nM£¬25 nM£¬15 nM£¬25 nM£¬ºÍ4 nM¡£Phase 1

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Aurora A (Human),25nM

Aurora B (Xenopus laevis),3nM

Aurora C (Human),15nM

MEK1,25nM

MEK2,4nM

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BI-847325¶ÔBRAFÍ»±äÐͺÍvemurafenibÄÍÒ©µÄºÚÉ«ËØÁöϸ°û±íÏÖ³öÉú³¤ÒÖÖÆ×÷Óã¬IC50 ·¶Î§Îª0.3 nM-2 μM£¬²¢·ÀÖ¹6¸öBRAFÍ»±äÐͺÚÉ«ËØÁöϸ°ûϵÖм¯ÂäÐγɡ£BI-847325Ò²»áͨ¹ý¼õÉÙMcl-1±í´ïÓÕµ¼Ï¸°ûµòÍö¡£[1]

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ÔÚ¸ººÉ1205LuºÍ1205LuRÒìÖÖÒÆÖ²ÎïµÄСÊóÖУ¬BI-847325 (75 mg/kg, p.o.)ÒýÆðÏÔÖøµÄÖ×ÁöÍË»¯£¬¶ø²»ÏÔÖø¸Ä±äÌåÖØ¡£[1]

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Cell lines: M229£¬M229R£¬A375£¬A375R£¬WM793£¬WM793R£¬1205Lu£¬1205LuR£¬M249£¬M249R£¬WM164£¬WM164R£¬WM39 ºÍ RPMI17951 ϸ°û

Concentrations: 30 μM

Incubation Time: 72 h

Method: ϸ°ûÒÔ2.5 × 103ϸ°û/100 μLµÄÃܶȽÓÖÖ£¬²¢Ê¹ÆäÉú³¤¹ýÒ¹£¬È»ºóÓÃÖð½¥Ôö¼ÓŨ¶ÈµÄBI-847325´¦Àí72СÊó¡£´úл»îÐÔʹÓÃAlamar blueÊÔ¼Á¸ù¾ÝÖÆÔìÉÌ·½°¸²â¶¨¡£

(Only for Reference)

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Animal Models: ¸ººÉ1205Lu ºÍ 1205LuR ÒìÖÖÒÆÖ²ÎïµÄСÊó

Formulation: 2-ôÇÒÒ»ùÏËάËØ£¬ÍÂΠ80£¬ÓÃ1 M HCl½«pH µ÷½Úµ½2.8

Dosages: 70 mg/kg

Administration: p.o.

(Only for Reference)

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[1] Phadke MS, et al. Mol Cancer Ther. 2015, 14(6), 1354-1364.

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