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942487-16-3

中文名稱 N-[2-[(1S,4R)-6-[[4-(環(huán)丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氫萘-1,4-亞氨-9-基]-2-氧代乙基]乙酰胺
英文名稱 PF-03814735
CAS 942487-16-3
分子式 C23H25F3N6O2
分子量 474.48
MOL 文件 942487-16-3.mol
更新日期 2024/11/15 18:20:32
942487-16-3 結構式 942487-16-3 結構式

基本信息

中文別名
N-[2-[(1S,4R)-6-[[4-(環(huán)丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氫萘-1,4-亞氨-9-基]-2-氧代乙基]乙酰胺
英文別名
CS-240
PF-03814735
PF-03814735 USP/EP/BP
RYYNGWLOYLRZLK-RBUKOAKNSA-N
N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]acetamide
Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-
所屬類別
生物化工:Aurora Kinase 抑制劑

物理化學性質

熔點181-183°C
密度1.443
儲存條件-20°C
溶解度在DMSO中的溶解度為20mg/mL,澄清
酸度系數(shù)(pKa)15.02±0.46(Predicted)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

常見問題列表

生物活性
PF-03814735是有效,有口服性,ATP 競爭性的,可逆的極光激酶A和B (aurora A/B) 的抑制劑,IC50值分別為0.8和5 nM。
靶點

Aurora 1

0.8 nM (IC 50 )

Aurora 2

5 nM (IC 50 )

Flt-1

10 nM (IC 50 )

FAK

22 nM (IC 50 )

TrkA

30 nM (IC 50 )

Met

100 nM (IC 50 )

FGFR1

100 nM (IC 50 )

體外研究

In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. Small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735.

體內研究

Once-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition. PF-03814735 is much more effective in NCI-H82 xenografts when administered on a weekly dosing schedule at 80 mg/kg compared with a daily schedule at 15 mg/kg. PF-03814735 delayed growth by 23.5 days on the weekly schedule, which corresponds to 0.9 logs of net cell kill during the course of treatment.

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