CCT365623 hydrochloride|2126136-98-7|-陌孚医药/Medlife

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CCT365623 hydrochloride

目录号: PL07500 纯度: ≥98%

CAS No. :2126136-98-7

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中文名称	CCT365623 hydrochloride
英文名称	CCT365623 hydrochloride
英文别名	CCT365623 (hydrochloride);BCP30916;CCT 365623 hydrochloride;CCT 365623 HCl; CCT365623 HCl;CCT365623 hydrochloride
Cas No.	2126136-98-7
分子式	C₁₈H₁₈ClNO₄S₃
分子量	443.99
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	CCT365623 hydrochloride 是具有口服活性的赖氨酰氧化酶 (LOX) 抑制剂，其IC₅₀ 值为0.89 μM。CCT365623 hydrochloride 通过驱动EGF抑制EGFR (pY1068) 和 AKT 的磷酸化。CCT365623 hydrochloride 具有极好的耐受性，良好的药理学特性。
生物活性	CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC 50 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.
性状	Solid
IC50 & Target[1][2]	IC50: 0.89 μM (LOX).
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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 T 1/2 PO of 0.6 h and F% (oral bioavailability) of 45%. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Tang H, et al. Author Correction: Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface. Nat Commun. 2019 Jul 18;10(1):3151.

溶解度数据	In Vitro: DMSO : 250 mg/mL (563.08 mM; Need ultrasonic)配制储备液

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