Doxycycline (hyclate)

CAS号

24390-14-5

分子式

C22H24N2O8·HCl·1/2C2H61/2H2O

主要靶点

Antibiotic|Antibacterial|MMP|ribosome

仅限科研使用

Cat No : CM02809

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Synonyms

Doxycycline|Doxycycline (hyclate)|Doxycycline hyclate|Doxycycline Hydrochloride|Doxycycline hydrochloride hemiethanolate hemihydrate|hyclate|inhibit|G55|Antibiotic|antibacterial activity|anti-proliferative activity|30S ribosome|293T|16S ribosome|Bacterial|Inhibitor|LNT-229|Matrix metalloproteinases|MCF 12A|MMP|WC 2031|WC2031|WC-2031|U343|SVG|盐酸强力霉素



产品信息

CAS号 24390-14-5
分子式 C22H24N2O8·HCl·1/2C2H61/2H2O
主要靶点 Antibiotic|Antibacterial|MMP|ribosome
主要通路 微生物学|蛋白酶体|微生物学|微生物学
分子量 512.9
纯度 100%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Doxycycline|Doxycycline (hyclate)|Doxycycline hyclate|Doxycycline Hydrochloride|Doxycycline hydrochloride hemiethanolate hemihydrate|hyclate|inhibit|G55|Antibiotic|antibacterial activity|anti-proliferative activity|30S ribosome|293T|16S ribosome|Bacterial|Inhibitor|LNT-229|Matrix metalloproteinases|MCF 12A|MMP|WC 2031|WC2031|WC-2031|U343|SVG|盐酸强力霉素

体内活性

方法:为检测体内抗肿瘤活性,将 Doxycycline hyclate (50 mg/kg) 腹腔注射给携带人乳腺癌肿瘤 4T1 的 BALB/c 小鼠,每天一次,持续十五天。 结果:Doxycycline 延迟肿瘤生长并降低肿瘤相关巨噬细胞和血管的数量。[3] 方法:为检测体内抗菌活性,将 Doxycycline hyclate (40 mg/kg) 腹腔注射给暴露于 B. pseudomallei 1026b 的 BALB/c 小鼠,每天两次,持续两周。 结果:用 Doxycycline 治疗的小鼠 100% 存活,并且从大多数存活小鼠的肺或脾脏中没有扩增出 B. pseudomallei 的 DNA。[4]

体外活性

方法:22 种肿瘤细胞用 Doxycycline hyclate 处理 48 h,使用 MTT 方法检测细胞活力。 结果:肺癌细胞对 Doxycycline 比其他大多数细胞系更敏感。NCI-H446 和 A549 细胞对 Doxycycline 敏感,IC50分别为 1.70 μM 和 1.06 μM。[1] 方法:人胰腺癌细胞 PANC-1 用 Doxycycline hyclate (10-40 μg/mL) 处理 8-24 h,使用 Flow Cytometry 方法检测细胞周期情况。 结果:Doxycycline 使细胞停滞在细胞周期的 G1-S 期。[2]

溶解度

H2O:13.89 mg/mL;DMSO:55 mg/mL (107.23 mM)

细胞实验

Doxycycline is diluted in culture medium at a concentration of 10 μg/mL. All in vitro treatments are performed in SMC cultures at 90% confluence, when ECM synthesis in SMC starts to be evident. Doxycycline (20 nM) is diluted in culture medium at a concentration of 10 μg/mL (20 nM), at which no toxicity or variation in primary cultured SMC proliferation has been reported, as well as in other cell lines and the incubation time is 48 h. SMC-C and SMC-Ch are seeded at equal cell density in 6-well plates and, when confluence reaches 90%, 1 mL culture medium is added to each well containing 3.7×104?Bq L-[5-3H]-proline (9.62×1011 Bq/mmol). After 48?h incubation, cells are lysed with 0.5 mL 0.5 mol/L NaOH for 1 h. The resulting solution is neutralized with an equal amount of 0.5 mol/L HCl, and 50 μL are used to measure total proteins with the Bradford method. One volume of 10% TCA is added to the remaining 250 μL and centrifuged at 13,000 g for 15?min at 4°C. The resulting precipitate is dissolved in 100 μL 0.2 mol/L NaOH, and then neutralized with 1 mol/L HCl. The solution is incubated with collagenase buffer (Tris-HCl, pH 7.6 20 mM, and CaCl2 250 mM final concentration) and 10 units of collagenase at 37°C overnight. Then, 150 μL 10% TCA are added and centrifuged at 13000 g for 15?min at 4°C. The resulting supernatant is added to 4 mL of scintillation fluid and the radioactivity is measured in a liquid scintillation counter LS 600 TA.

参考文献

1.Qin Y, et al. Doxycycline reverses epithelial-to-mesenchymal transition and suppresses the proliferation and metastasis of lung cancer cells. Oncotarget. 2015 Dec 1;6(38):40667-79.
2.Son K, et al. Doxycycline induces apoptosis in PANC-1 pancreatic cancer cells. Anticancer Res. 2009 Oct;29(10):3995-4003.
3.Tang X, et al. Doxycycline attenuates breast cancer related inflammation by decreasing plasma lysophosphatidate concentrations and inhibiting NF-κB activation. Mol Cancer. 2017 Feb 8;16(1):36.
4.Gelhaus HC, et al. Efficacy of post exposure administration of doxycycline in a murine model of inhalational melioidosis. Sci Rep. 2013;3:1146.
5.Meijer LA, et al. Vet Q, 1993, 15(1), 1-5.

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