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 activelysyl oxidase (LOX)inhibitor, with anIC50of 0.89 μM. CCT365623 hydrochloride suppressesEGFR(pY1068) andAKTphosphorylation driven byEGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties[1]. |
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体外研究
(In Vitro) | CCT365623 inhibits LOX at ~5 μM in the biosensor system[1].
CCT365623 (0-40 μM) concentration-dependently decreases the protein levels of surface EGFR[1].
CCT365623 (5 μM) decreases the protein levels of pY1068 EGFR, pAKT and MATN2, and increases the protein levels of pSMAD2[1].
CCT365623 disrupts HTRA1 multimerization, activates TGFβ1 signalling, suppresses MATN2 expression, suppresses EGFR surface retention, and suppresses EGFR signalling[1].
Western Blot Analysis[1] | Cell Line: | MDA-MB-231 cells. | | Concentration: | 0-40 μM. | | Incubation Time: | 24 hours | | Result: | Significantly decreased the protein levels of surface EGFR, pY1068 EGFR, pAKT and MATN2.
Increased the protein levels of pSMAD2. |
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体内研究
(In Vivo) | CCT365623 displays good stability in mouse liver microsomes and does not inhibit the cardiac potassium channel hERG[1].
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[1].
CCT365623 exhibits a T1/2PO of 0.6 h and F% (oral bioavailability) of 45%[1].
| Animal Model: | Mouse model of spontaneous breast cancer that metastasizes to the lungs (70 days old)[1]. | | Dosage: | 70 mg/kg. | | Administration: | Oral gavage per day for about 3 weeks. | | Result: | Significantly reducedMATN2protein 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(563.08 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2523 mL | 11.2615 mL | 22.5230 mL | | 5 mM | 0.4505 mL | 2.2523 mL | 4.5046 mL | | 10 mM | 0.2252 mL | 1.1262 mL | 2.2523 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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