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| 1mg |
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| 10mg |
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Purity: ≥98%
PX-478 2HCl (PX-478 dihydrochloride) is a novel, potent and orally bioactive inhibitor of HIF-1α (hypoxia-inducible factor-1α) with potential antitumor activity. PX-478 has excellent in vivo antitumor activity, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 has high water solubility, good i.v., i.p. and p.o. antitumor activity.
| ln Vitro |
PX-478 was applied to HIF-1α protein-expressing PC3 and DU 145 cells for 20 hours at normoxic conditions. PX-478 had a greater effect on PC3 cells than DU 145 cells. According to densitometric analysis, PC3 cells suppressed HIF-1α with an IC50 of 20–25 μM under normoxic circumstances, whereas DU inhibited HIF-1α with an IC50 of 40–50 μM. Different concentrations of PX-478 (10, 20, 30, 40, 50, and 60 μM) were applied to PC3 and DU 145 cells under normoxic or hypoxic conditions for a duration of 18 to 20 hours. PC3 cells were more sensitive to PX-478 than DU 145 cells in normoxic conditions. Clonogenic viability for PC3 cells (n=3) and DU 145 cells with IC50 values of 17 μM and 35 μM, respectively. The drug's half-life (IC50) for PC3 cells was 16 μM and for DU 145 cells it was 22 μM when the cells were treated for eighteen hours under hypoxic circumstances. Consequently, in hypoxic settings, DU 145 cells are more susceptible to PX-478 [1].
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| ln Vivo |
For two weeks after birth, (Nfatc1-Cre/caACVR1fl/fl) mice with congenital heart disease received PX-478 every other day. The amount of ectopic bone in treated mice's ankle joints was significantly less (6.8 mm3 vs. 2.2 mm3, P<0.01) when compared to mutant mice that received vehicle treatment[2].
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| Animal Protocol |
Mice bearing MCF-7 human breast cancer, HT-29 colon cancer, PC-3 prostate cancer, DU-145 prostate cancer, OvCar-3 ovarian cancer, A-549 non-small cell lung cancer, SHP-77 small cell lung cancer, and Caki-1 renal cancer, Panc-1, MiaPaCa, or BxPC-3 pancreatic cancer xenografts.;
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| References |
[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 |
| Molecular Formula |
C13H20CL4N2O3
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|---|---|
| Molecular Weight |
392.0230
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| CAS # |
685898-44-6
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| Related CAS # |
685898-44-6 (HCl);685847-78-3;
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| SMILES |
[O-][N+](CCCl)(CCCl)C(C=C1)=CC=C1C[C@H](N)C(O)=O.Cl.Cl
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| Synonyms |
PX478; PX-478; PX 478; PX478 HCl;PX478 Hydrochloride;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 78 mg/mL (197.9 mM)
Water:78 mg/mL (197.9 mM)
Ethanol: N/A
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| Solubility (In Vivo) |
10% DMSO: 40% PEG300: 5% Tween-80: 45% Saline: ≥ 5 mg/mL (12.7 mM) (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5509 mL | 12.7545 mL | 25.5089 mL | |
| 5 mM | 0.5102 mL | 2.5509 mL | 5.1018 mL | |
| 10 mM | 0.2551 mL | 1.2754 mL | 2.5509 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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