»ù±¾ÐÅÏ¢
·Ö×Óʽ | C29H28N4O2 |
·Ö×ÓÁ¿ | 464.56 |
´æ´¢Ìõ¼þ | Freezer -20¡æ |
²úÆ·ÃèÊö
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
°Ðµã£¨IC50 & Targe£©
Aurora A (Human),25nM
Aurora B (Xenopus laevis),3nM
Aurora C (Human),15nM
MEK1,25nM
MEK2,4nM
ÌåÍâÑо¿
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]
ÌåÄÚÑо¿
ÔÚ¸ººÉ1205LuºÍ1205LuRÒìÖÖÒÆÖ²ÎïµÄСÊóÖУ¬BI-847325 (75 mg/kg, p.o.)ÒýÆðÏÔÖøµÄÖ×ÁöÍË»¯£¬¶ø²»ÏÔÖø¸Ä±äÌåÖØ¡£[1]
ϸ°ûʵÑé
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)
¶¯ÎïʵÑé
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)
²Î¿¼ÎÄÏ×
[1] Phadke MS, et al. Mol Cancer Ther. 2015, 14(6), 1354-1364.
°ÙÁéÍþ¿Æ¼¼