产品
编 号：F457118
分子式：C20H17F3N4O3
分子量：418.37
分子式：C20H17F3N4O3
分子量：418.37
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 778277-15-9
产品详情
生物活性：
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 μM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.
体内研究：
GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters.GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses.GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo.Animal Model:Male Balb/c mice
Dosage:5 mg/kg, 20 mg/kg
Administration:5 mg/kg intravenously or 20 mg/kg orally
Result: AUC_inf (min*ug/mL)292.37
AUC_inf (hrs*nM11647
Cmax(nM)4386.08
Tmax(hrs)0.50
Clast (nM)636.16
T1/2(hrs)2.30
Vss(L/kg)9.18
F (%)44.82
Animal Model:p210 xenograft model
Dosage:50 or 100 mg/kg
Administration:oral, twice daily, for 7 days
Result:Could normalize blood counts and spleen size.
Animal Model:Bone marrow transduction/transplantation model
Dosage:75 mg/kg
Administration:twice daily
Result:Showed no significant response (alone).Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.
体外研究：
GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 μM but no inhibition for myristate site mutant E505K (IC50 ＞10 μM).
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 μM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.
体内研究：
GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters.GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses.GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo.Animal Model:Male Balb/c mice
Dosage:5 mg/kg, 20 mg/kg
Administration:5 mg/kg intravenously or 20 mg/kg orally
Result: AUC_inf (min*ug/mL)292.37
AUC_inf (hrs*nM11647
Cmax(nM)4386.08
Tmax(hrs)0.50
Clast (nM)636.16
T1/2(hrs)2.30
Vss(L/kg)9.18
F (%)44.82
Animal Model:p210 xenograft model
Dosage:50 or 100 mg/kg
Administration:oral, twice daily, for 7 days
Result:Could normalize blood counts and spleen size.
Animal Model:Bone marrow transduction/transplantation model
Dosage:75 mg/kg
Administration:twice daily
Result:Showed no significant response (alone).Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.
体外研究：
GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 μM but no inhibition for myristate site mutant E505K (IC50 ＞10 μM).
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备