PX-478 2HCl

Name: PX-478 2HCl
SKU: GC11031
Availability: InStock
Rating: 5 (30 reviews)

目录号 : GC11031

PX-478是一种选择性抑制剂，可以抑制常规和低氧诱导的HIF-1α水平。

PX-478 2HCl Chemical Structure

Cas No.:685898-44-6

规格价格库存购买数量

10mM (in 1mL DMSO)	¥693.00	现货
5mg	¥599.00	现货
10mg	¥1,050.00	现货
50mg	¥2,405.00	现货
100mg	¥3,938.00	现货

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Sample solution is provided at 25 µL, 10mM.

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Description

PX-478 is a selective inhibitor that suppresses constitutive and hypoxia-induced HIF-1α levels. PX-478 inhibits HIF-1α at multiple levels including inhibition of HIF-1α translation and reduction in HIF-1α mRNA levels.^[1] PX-478 also has been shown antitumor activity against several aggressive human tumor xenografts.^[2]

In vitro and in vivo study demonstrated that PX-478 could inhibit normoxic and hypoxia-induced HIF-1α expression as well as inflammatory molecule COX-2 and immunosuppressive molecule PD-L1 expression. Therefore, PX-478 shows a wide effect on tumor development, such as suppressing proliferation, promoting cells apoptosis, inhibiting EMT process and arresting cell cycle. In vivo experiment indicated the inhibitory effect of PX-478 on tumor growth. ^[1]

References:
[1].Zhu Y, et al. Inhibition of HIF-1α by PX-478 suppresses tumor growth of esophageal squamous cell cancer in vitro and in vivo. Am J Cancer Res. 2017 May 1;7(5):1198-1212.
[2].Palayoor ST, et al. PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer. 2008 Nov 15;123(10):2430-7.

PX-478是一种选择性抑制剂，可以抑制常规和低氧诱导的HIF-1α水平。PX-478在多个层面上抑制HIF-1α，包括抑制HIF-1α翻译和降低HIF-1α mRNA水平。^[1]此外，PX-478还显示出对几种侵袭性人类肿瘤异种移植的抗肿瘤活性。^[2]

体外和体内研究表明，PX-478可以抑制正常氧和低氧诱导的HIF-1α表达以及炎性分子COX-2和免疫抑制分子PD-L1的表达。因此，PX-478对肿瘤发展具有广泛影响，如抑制增殖、促进细胞凋亡、抑制EMT过程并阻止细胞周期。体内实验显示了PX-478对肿瘤生长的抑制作用。^[1]

实验参考方法

Cell experiment [1]:
Cell lines	EC109 and EC9706 cell lines
Preparation Method	Both cell lines were cultured in RPMI 1640 supplemented with 10% FBS at 37°C in a 5% CO2 humidified incubator. Cells were starved for 24 h in medium containing 0.1% FBS prior to treatment.
Reaction Conditions	PX-478 was added to the cultures to a final concentration of 20 umol/L after serum starvation overnight.
Applications	PX-478 could inhibit normoxic and hypoxia-induced HIF-1α expression as well as COX-2 and PD-L1 expression in vitro at a dose of 20 μM in EC9706 and EC109 cells. Targeted HIF-1α can effectively reduce their expression.
Animal experiment [1]:
Animal models	6-week-old female BALB/c nude mice, 18 ± 2 g, SPF grade
Preparation Method	EC109 cells were re-suspended in PBS at 10⁷/mL. A total of 12 BABL/c nude female mice were used. Mice were injected with EC109 cells in the right flank area to establish the tumor xenograft. The 12 tumor-bearing mice in each group were randomly divided into the control group and the PX-478 groups. All the drugs were delivered via p.o. gavage administration.
Dosage form	30 mg/kg every other day
Applications	PX-478 shows a wide effect on tumor development, such as suppressing proliferation, promoting cells apoptosis, inhibiting EMT process and arresting cell cycle. In vivo mouse xenograft models showed the inhibitory effect on tumor growth. In addition, it can reduce COX-2 and PD-L1 expression.
References: [1].Zhu Y, et al. Inhibition of HIF-1α by PX-478 suppresses tumor growth of esophageal squamous cell cancer in vitro and in vivo. Am J Cancer Res. 2017 May 1;7(5):1198-1212.

化学性质

Cas No.	685898-44-6	SDF
化学名	(S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide dihydrochloride
Canonical SMILES	ClCC[N+](C1=CC=C(C[C@@](N)([H])C(O)=O)C=C1)([O-])CCCl.Cl.Cl
分子式	C₁₃H₂₀Cl₄N₂O₃	分子量	394.12
溶解度	79mg/mL in DMSO (200.45mM), 79mg/mL in Water (200.45mM), 79mg/mL in Ethanol (200.45mM)	储存条件	Store at -20°C, stored under nitrogen, away from moisture
General tips	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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。
Shipping Condition	评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。