产品
编 号：F741687
分子式：C23H18ClFN6O2
分子量：464.88
分子式：C23H18ClFN6O2
分子量：464.88
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2630904-45-7
产品详情
生物活性：
MRTX-1719 is a potent, orally active, selective PRMT5?MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5?MTA and PRMT5. MRTX-1719 binds to the PRMT5?MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.
体内研究：
MRTX1719 (12.5-100 mg/kg/每天，口服，21天) 可降低 Lu-99 原位异种移植肿瘤的生长。药代动力学分析ModelRouteDose (mg/kg)Cltotal (mL/min/kg)Vdss (L/kg)t1/2 (h)
CD-1 mouse.i.v.3 836.31.5
Beagle dogi.v.2 143.44.8
Cynomolgus monkeyi.v. 2 152.36.1
ModelRouteDose (mg/kg)Cmax (ug/mL)AUCinf (h*ug/mL)F (%)
CD-1 mouse.p.o.301.164.8580
Beagle dogp.o.10 1.407.4759
Cynomolgus monkeyp.o. 10//41
Animal Model:Lu-99 (an MTAP/CDKN2A-deleted human lung cancer cell line ) xenograft tumor modelsDosage:12.5, 25, 50, and 100 mg/kg/d, 21 day
Administration:Oral gavage
Result:Reduced the tumor volume with 86% tumor growth inhibition (TGI) at 50 mg/kg and 88% TGI at 100 mg/kg.
体外研究：
MRTX-1719 (10 天) 在 MTAP 缺失的 HCT116 细胞而非野生型细胞中抑制 PRMT5 活性，IC50 为 8 nM。MRTX1719 (10 天) 在 MTAP 敲除的 HCT116 细胞中的 IC50 值为 12 nM，对野生型 HCT116 细胞的 IC50 值为 890 nM。
MRTX-1719 is a potent, orally active, selective PRMT5?MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5?MTA and PRMT5. MRTX-1719 binds to the PRMT5?MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.
体内研究：
MRTX1719 (12.5-100 mg/kg/每天，口服，21天) 可降低 Lu-99 原位异种移植肿瘤的生长。药代动力学分析ModelRouteDose (mg/kg)Cltotal (mL/min/kg)Vdss (L/kg)t1/2 (h)
CD-1 mouse.i.v.3 836.31.5
Beagle dogi.v.2 143.44.8
Cynomolgus monkeyi.v. 2 152.36.1
ModelRouteDose (mg/kg)Cmax (ug/mL)AUCinf (h*ug/mL)F (%)
CD-1 mouse.p.o.301.164.8580
Beagle dogp.o.10 1.407.4759
Cynomolgus monkeyp.o. 10//41
Animal Model:Lu-99 (an MTAP/CDKN2A-deleted human lung cancer cell line ) xenograft tumor modelsDosage:12.5, 25, 50, and 100 mg/kg/d, 21 day
Administration:Oral gavage
Result:Reduced the tumor volume with 86% tumor growth inhibition (TGI) at 50 mg/kg and 88% TGI at 100 mg/kg.
体外研究：
MRTX-1719 (10 天) 在 MTAP 缺失的 HCT116 细胞而非野生型细胞中抑制 PRMT5 活性，IC50 为 8 nM。MRTX1719 (10 天) 在 MTAP 敲除的 HCT116 细胞中的 IC50 值为 12 nM，对野生型 HCT116 细胞的 IC50 值为 890 nM。
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