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標(biāo)簽:Chloropyramine hydrochloride
聯(lián)系人:高小姐
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化學(xué)性質(zhì):
規(guī)格 | 10mM*1mLinDMSO 50mg |
CAS | 6170-42-9 |
別名 | N/A |
化學(xué)名 | N/A |
分子式 | C16H21Cl2N3 |
分子量 | 326.26 |
溶解度 | DMSO : 30 mg/mL (91.95 mM) |
儲(chǔ)存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
BT474 cells are highly sensitive to Chloropyramine hydrochloride (compound 1) treatment, whereby 1 μM concentrations cause a 40% reduction of viability after 48 h of treatment. It is found that at 1 μM concentrations of Chloropyramine hydrochloride, viability of control MCF7-pcDNA3 cells is significantly higher than the viability of MCF7-VEGFR-3 cells (P<0.01) and at 10 μM concentration this difference reaches twofold (P<0.001). In the BT474 cells treatment with Chloropyramine hydrochloride also leads to a concentration-dependent decrease of cell proliferation. When treatment with Chloropyramine hydrochloride is continued for 48 h, the breast cancer cells that overexpressed VEGFR-3 undergo apoptosis. This effect is dose-dependent, with 10 μM Chloropyramine hydrochloride inducing apoptosis in more than 60% of BT474 cells. In our model cell lines MCF7-pcDNA3 and MCF7-VEGFR-3, treatment with 10 μM Chloropyramine hydrochloride for 48 h leads to a 4-fold increase in apoptotic cell death in the cell line that overexpressed VEGFR-3 (18% versus 76 % respectively)[1].
Chloropyramine hydrochloride causes a dramatic reduction of tumor growth in both model systems whereby the tumor size in the treated groups is approximately 20% of the tumor size in vehicle control groups. Doxorubicin administered at 3 mg/kg causes approximately 60% reduction of tumor growth, but has no effect on tumor growth at 0, 3 mg/kg. In contrast, there is a modest effect of Chloropyramine hydrochloride alone (50% reduction of tumor growth). The low-dose combination of Chloropyramine hydrochloride and doxorubicin has a prolonged anti-tumor effect (85% reduction of tumor growth) that is greater than either drug alone[1].
[1]. Kurenova EV, et al. Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo. J Med Chem. 2009 Aug 13;52(15):4716-24.
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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國(guó)銀行山東省分行營(yíng)業(yè)部
賬 號(hào):2169 2341 6278