{{cart_num}}
My CartCAS：685898-44-6
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Yellow to brown Solid
Qty：
Size：
| CAS | 685898-44-6 |
| Name | PX-478 2HCl |
| Molecular Formula | C13H20Cl4N2O3 |
| Molecular Weight | 394.12 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | Yellow to brown Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD11840749 |
| SMILES | [O-][N+](CCCl)(CCCl)C(C=C1)=CC=C1C[C@H](N)C(O)=O.Cl.Cl |
| Target Point | HIF/HIF Prolyl-Hydroxylase |
| Passage | HIF |
| Background | PX-478 is a hypoxia-inducible factor-1α (HIF-1α) inhibitor with anticancer activity. |
| Biological Activity | PX-478 是有抗癌活性的缺氧诱导因子-1α (HIF-1α) 抑制剂，对一些癌细胞系 IC50 为 20-30 μM[1-2]。 |
| In Vitro | PC3和DU145细胞表达HIF-1α蛋白在常氧条件下用PX-478处理20小时。与DU145细胞相比，PC3细胞对PX-478更敏感。光密度分析显示，在常氧条件下对PC3细胞的HIF-1α抑制的IC 50为20-25μM，而对于DU 145细胞的HIF-1α抑制的IC 50为40-50μM。在常氧或缺氧条件下，用不同浓度的PX-478(10，20，30，40，50和60μM)处理PC3和DU145细胞18-20小时。在常氧条件下，PC3细胞对PX-478比对DU145细胞更敏感。对于PC3细胞，克隆形成存活(n = 3)的IC50为17μM，对于DU145细胞为35μM。当细胞在低氧条件下用药物处理18小时时，PC3细胞的IC50为16μM，DU145细胞的IC50为22μM。因此DU145细胞在低氧条件下对PX-478更敏感[1]。 |
| In Vivo | PX-478从出生开始每隔一天给予患有先天性HO(Nfatc1-Cre/caACVR1fl/fl)的小鼠2周。与用载体处理的突变小鼠相比，经处理的小鼠在踝关节处的异位骨显著减少(6.8 mm3对2.2 mm3，P <0.01)[2]。 |
| Cell Experiment | 为了确定PX-478与辐射组合的作用，在常氧条件下用PX-478处理细胞24小时，照射并在1小时后铺板。 12天后菌落用结晶紫染色，计数> 50个细胞的菌落。[1]。 |
| Animal Experiment | 小鼠[2]通过腹膜内注射给PBS溶液中的PX-478(100mg/kg)或雷帕霉素(5mg/kg)施用烧伤/腱切断或杂交HO小鼠。在研究期间，小鼠每隔一天接受注射，总共2周。 |
| Data Literature Source | [1]. 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):2430-2437. [2]. Agarwal S，et al. Inhibition of Hif1α prevents both trauma-induced and genetic heterotopic ossification. Proc Natl Acad Sci U S A. 2016 Jan 19;113(3):E338-47 |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg 50mg |
PX-478 是有抗癌活性的缺氧诱导因子-1α (HIF-1α) 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Manual Download
