产品
编 号：F620521
分子式：C22H24N4O3S
分子量：424.52
分子式：C22H24N4O3S
分子量：424.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 2173556-69-7
产品详情
生物活性：
PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis.
体内研究：
PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome.PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis.Animal Model:C57BL/6 mice
Dosage:5 mg/kg, 25 mg/kg
Administration:5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days
Result:Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg.
Animal Model:C57BL/6 mice
Dosage:2 mg/kg, 10 mg/kg
Administration:2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days
Result:PO (Gavage)IV (Bolus)
Tmax (hr)0.5
Cmax (ng/mL)2423
AUC0-24 (ng/mL?hr)48211588
AUCINF (ng/mL?hr)48971590
t1/2 (hr)1.31.0
MRT (hr)1.80.8
CL (mL/hr/kg)1258
CL (mL/min/kg)21
Vss (mL/kg)1009
Vss (L/kg)1.0
F(%)61
Animal Model:C57BL/6 mice
Dosage:1 mg/kg
Administration:1 mg/kg, i.p.
Result:Providedeffective protection against TNFα-induced lethal shock.
Animal Model:C57BL/6 mice
Dosage:5 mg/kg
Administration:5 mg/kg, i.v.
Result:Significantly reduced the numberof pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigrationof RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate andinvasion ability of B16-F10 or RFP-LL/2 cells without theendothelial cell monolayer in vitro.
体外研究：
PK68 has highly potent inhibition of TNF-induced necroptosis with EC50 values of 23 nM and 13 nM in human and mouse cells, respectively.PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC50 value of 90 nM.PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation.
PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis.
体内研究：
PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome.PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis.Animal Model:C57BL/6 mice
Dosage:5 mg/kg, 25 mg/kg
Administration:5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days
Result:Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg.
Animal Model:C57BL/6 mice
Dosage:2 mg/kg, 10 mg/kg
Administration:2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days
Result:PO (Gavage)IV (Bolus)
Tmax (hr)0.5
Cmax (ng/mL)2423
AUC0-24 (ng/mL?hr)48211588
AUCINF (ng/mL?hr)48971590
t1/2 (hr)1.31.0
MRT (hr)1.80.8
CL (mL/hr/kg)1258
CL (mL/min/kg)21
Vss (mL/kg)1009
Vss (L/kg)1.0
F(%)61
Animal Model:C57BL/6 mice
Dosage:1 mg/kg
Administration:1 mg/kg, i.p.
Result:Providedeffective protection against TNFα-induced lethal shock.
Animal Model:C57BL/6 mice
Dosage:5 mg/kg
Administration:5 mg/kg, i.v.
Result:Significantly reduced the numberof pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigrationof RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate andinvasion ability of B16-F10 or RFP-LL/2 cells without theendothelial cell monolayer in vitro.
体外研究：
PK68 has highly potent inhibition of TNF-induced necroptosis with EC50 values of 23 nM and 13 nM in human and mouse cells, respectively.PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC50 value of 90 nM.PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation.
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