产品
编 号：F271881
分子式：C18H18ClNO4S3
分子量：443.99
分子式：C18H18ClNO4S3
分子量：443.99
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2126136-98-7
产品详情
生物活性：
CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.
体内研究：
CCT365623 displays good stability in mouse liver microsomes and does not inhibit the cardiac potassium channel hERG.CCT365623 (70 mg/kg, oral gavage per day) significantly delays the development of the primary tumors and also suppresses metastatic lung burden in the animals. CCT365623 disrupts EGFR cell surface retention and delays the growth of primary and metastatic tumor cell.CCT365623 exhibits a T1/2PO of 0.6 h and F% (oral bioavailability) of 45%.Animal Model:Mouse model of spontaneous breast cancer that metastasizes to the lungs (70 days old).
Dosage:70 mg/kg.
Administration:Oral gavage per day for about 3 weeks.
Result:Significantly reduced MATN2 protein levels in both the primary and metastatic lung tumors and this is accompanied by the loss of EGFR from the plasma membranes of the cells in both the primary and metastatic tumors.
体外研究：
CCT365623 inhibits LOX at ~5 μM in the biosensor system.CCT365623 (0-40 μM) concentration-dependently decreases the protein levels of surface EGFR.CCT365623 (5 μM) decreases the protein levels of pY1068 EGFR, pAKT and MATN2, and increases the protein levels of pSMAD2.CCT365623 disrupts HTRA1 multimerization, activates TGFβ1 signalling, suppresses MATN2 expression, suppresses EGFR surface retention, and suppresses EGFR signalling.
CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.
体内研究：
CCT365623 displays good stability in mouse liver microsomes and does not inhibit the cardiac potassium channel hERG.CCT365623 (70 mg/kg, oral gavage per day) significantly delays the development of the primary tumors and also suppresses metastatic lung burden in the animals. CCT365623 disrupts EGFR cell surface retention and delays the growth of primary and metastatic tumor cell.CCT365623 exhibits a T1/2PO of 0.6 h and F% (oral bioavailability) of 45%.Animal Model:Mouse model of spontaneous breast cancer that metastasizes to the lungs (70 days old).
Dosage:70 mg/kg.
Administration:Oral gavage per day for about 3 weeks.
Result:Significantly reduced MATN2 protein levels in both the primary and metastatic lung tumors and this is accompanied by the loss of EGFR from the plasma membranes of the cells in both the primary and metastatic tumors.
体外研究：
CCT365623 inhibits LOX at ~5 μM in the biosensor system.CCT365623 (0-40 μM) concentration-dependently decreases the protein levels of surface EGFR.CCT365623 (5 μM) decreases the protein levels of pY1068 EGFR, pAKT and MATN2, and increases the protein levels of pSMAD2.CCT365623 disrupts HTRA1 multimerization, activates TGFβ1 signalling, suppresses MATN2 expression, suppresses EGFR surface retention, and suppresses EGFR signalling.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备