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PX-478

Catalog No. T6961 CAS 685898-44-6

Synonyms: PX-478 2HCl

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PX-478, CAS 685898-44-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 48.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 215.00
50 mg	In stock	$ 291.00
100 mg	In stock	$ 457.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99.79%

Purity: 97.93%

Purity: 97%

Biological Description

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Storage & Solubility Information

Description	PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.
In vitro	METHODS: Tumor cells MCF-7, HT-29 and PC-3 were treated with PX-478 under normoxic or hypoxic conditions for 16 h, and then grown under normoxic conditions for another 56 h. Cell viability was detected by MTT assay. RESULTS: PX-478 produced a smaller but significantly greater inhibition of cell growth under hypoxic conditions compared to normoxic conditions. the hypoxic/normoxic IC50 of MCF-7 cells was 25.1/20.0 µM, with a ratio of 1.25. the hypoxic/normoxic IC50 of HT-29 cells was 29.5/23.9 µM, with a ratio of 1.20, and that of PC-3 cells was 16.2/11.9 µM, with a ratio of 16.2/11.0 µM. IC50 for PC-3 cells was 16.2/11.1 µM with a ratio of 1.45. [1] METHODS: Human prostate cancer cells PC3 and DU 145 were treated with PX-478 (10-40 µM) under normoxic conditions for 20 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Under normoxic conditions, the IC50 of PX-478 for HIF-1α inhibition in PC3 cells was 20-25 µM (ΔHIF:0.56±0.08), while the IC50 of HIF1α inhibition in DU 145 cells was 40-50 µM (ΔHIF:0.47±0.08). [2]
In vivo	METHODS: To study the activity on metabolism in vivo, PX-478 (5 mg/kg) was administered by gavage to C57BL/6 mice on a high-fat diet (HFD) every two days for seven weeks. RESULTS: PX-478 treatment effectively inhibited HFD-induced HIF1α activation in adipose tissue. Inhibition of HIF1α in adipocytes significantly improved metabolism. [3] METHODS: In order to detect the anti-tumor activity in vivo, PX-478 (75-100 mg/kg) was intraperitoneally injected into scid mice carrying tumors OvCar-3, SHP-77, MCF-7, or PC-3 once a day for five days. RESULTS: PX-478 showed antitumor activity against established human tumor xenografts. [4]
Cell Research	PX-478 is prepared as a 10 mM stock in distilled water and used immediately[1]. To determine the effect of PX-478 in combination with radiation, cells are treated with PX-478 for 24 hr under normoxic condition, irradiated and plated after 1 hr. Colonies are stained with crystal violet after 12 days and the colonies of >50 cells are counted. For combination treatments, net survival is calculated by correcting the toxicity of PX-478 alone. Enhancement factor (EF) is calculated by dividing the dose of radiation required to reduce plating efficiency to 10% when cells are treated with radiation alone by the dose of radiation required to reduce plating efficiency to 10% when cells are treated with PX-478 and radiation[1].

Synonyms	PX-478 2HCl
Molecular Weight	394.12
Formula	C13H20Cl4N2O3
CAS No.	685898-44-6

Storage

store at low temperature,keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (126.86 mM)

H2O: 88.81mM

References and Literature

1. Koh MY, et al. Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2008 Jan;7(1):90-100. 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. 3. Sun K, et al. Selective inhibition of hypoxia-inducible factor 1α ameliorates adipose tissue dysfunction. Mol Cell Biol. 2013 Mar;33(5):904-17. 4. Welsh S, et al. Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2004 Mar;3(3):233-44.

Citations

1. Chang L L, Lu P H, Yang W, et al. AKR1C1 promotes non-small cell lung cancer proliferation via crosstalk between HIF-1α and metabolic reprogramming. Translational Oncology. 2022, 20: 101421 2. Liu R, Tian Y, Wang J, et al.Visible light–initiated radical 1,3-difunctionalization of β, γ-unsaturated ketones.Science Advances.2022, 8(49): eabq8596.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Angiogenesis related Compound Library Anti-Aging Compound Library Target-Focused Phenotypic Screening Library HIF-1 Signaling Pathway Compound Library Anti-Cancer Metabolism Compound Library

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Glucosamine dencichine AKB-6899 AKBA Hydralazine hydrochloride M1001 IDF-11774 Chlorogenic Acid

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Keywords

PX-478 685898-44-6 Angiogenesis Autophagy Chromatin/Epigenetic Metabolism HIF HIF/HIF Prolyl-Hydroxylase Inhibitor HIFs inhibit HIF-PH PX-478 2HCl Hypoxia-inducible factors PX478 PX 478 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.