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抑制剂/激活剂

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凋亡与自噬

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PX-478

PX-478 是一种具有口服活性的 HIF-1α 抑制剂，并具有抗癌活性。PX-478 可穿透血脑屏障。

货号：
TK0561
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	685898-44-6
生物活性	PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
分子式	C13H20Cl4N2O3
分子量	394.12
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	-20°C, stored under nitrogen, away from moisture
溶解性数据	DMSO : 100 mg/mL (253.73 mM; Need ultrasonic) H2O : ≥ 35 mg/mL (88.81 mM)
体内研究	PX-478 is administered to mice with congenital HO (Nfatc1-Cre/caACVR1) every other day starting from birth for 2 wk. Treated mice have significantly less ectopic bone at the ankle joints compared with mutant mice treated with vehicle (6.8 mm vs. 2.2 mm, P<0.01).
体外研究	PC3 and DU 145 cells express HIF-1α protein are treated with PX-478 for 20 hr under normoxia. PC3 cells are more sensitive to PX-478 as compared with DU 145 cells. Densitometric analysis shows that the IC50 for HIF-1α inhibition for PC3 cells under normoxic condition is 20-25 μM, whereas the IC50 for HIF-1α inhibition for the DU 145 cells is 40-50 μM. PC3 and DU 145 cells are treated with different concentrations of PX-478 (10, 20, 30, 40, 50, and 60 μM) for 18-20 hr under normoxia or hypoxia. Under normoxia, PC3 cells are more sensitive to PX-478 than DU 145 cells. IC50 for clonogenic survival (n=3) is 17 μM for PC3 cells and 35 μM for DU 145 cells. When cells are treated with the drug under hypoxic condition for 18 hr, the IC50 is 16 μM for PC3 cells and 22 μM for DU 145 cells. Thus DU 145 cells are more sensitive to PX-478 under hypoxic condition.
文献	•Circulation. 2020 Jul 28;142(4):384-400. •Sci Transl Med. 2020 Apr 8;12(538):eaay1620. •Acta Pharm Sin B. 14 October 2021. •Front Immunol. 2018 Jul 23;9:1667. •Mol Nutr Food Res. 2018 Aug;62(16):e1800164. •J Biol Chem. 2017 Jun 30;292(26):11009-11020. •Arch Biochem Biophys. 2019 Jul 30;670:94-103. •Biochem Biophys Res Commun. 2021 Aug 3;572:72-79. •Iran J Basic Med Sci. 2020 Jun;23(6):819-825. •Research Square Preprint. 2021 Dec.
纯度及产品资料	≥98%

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