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PX-478 2HCl Catalog No.GC11031

HIF-1α inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$66.00
In stock
5mg
$57.00
In stock
10mg
$100.00
In stock
50mg
$229.00
In stock
100mg
$375.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

DU145 cells

Preparation method

The solubility of this compound in DMSO is > 19.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

25 μM; 18 hrs

Applications

Under hypoxic condition, incubation with PX-478 for 18 hrs increased the radiosensitivity of DU145 cells, but did not significantly affect HIF-1α protein level.

Animal experiment [2]:

Animal models

Nu/nu mice bearing C6 reporter xenografts

Dosage form

30 mg/kg; p.o.; for 2 days

Applications

In nu/nu mice bearing C6 reporter xenografts, PX-478 treatment (30 mg/kg; p.o.; for 2 days) inhibited the transcriptional activity of HIF-1 in central ischemic regions of C6 tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Palayoor ST, Mitchell JB, Cerna D, et al. PX-478, an inhibitor of hypoxia-inducible factor-1α, enhances radiosensitivity of prostate carcinoma cells. International journal of cancer, 2008, 123(10): 2430-2437.

[2]. Schwartz DL, Powis G, Thitai-Kumar A, et al. The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Molecular cancer therapeutics, 2009, 8(4): 947-958.

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Chemical Properties

Cas No. 685898-44-6 SDF
Chemical Name (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
Formula C13H20Cl4N2O3 M.Wt 394.12
Solubility ≥19.7mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PX-478 2HCl, also called PX-478, is an experimental HIF-1α inhibitor. It inhibited HIF-1α protein at multiple levels in cancer cell lines under normoxia and hypoxia with an IC50 value of ~20-30 μM [1].

Hypoxia-inducible transcription factor HIF-1α activates target genes involved in glycolysis, erythropoiesis and angiogenesis. HIF-1α also regulates the expression of genes coding for apoptotic pathway, growth factors/receptors, cell cycle regulators, metastasis and invasiveness [1].

Under normoxic condition, the IC50 for PX-478 to inhibit HIF-1α in PC3 cells was 20-25 μmol/L, whereas the IC50 for PX-478 to inhibit HIF-1α in the DU 145 cells was ~40-50 μmol/L. in both DU 145 and PC3 cells, 1-hr hypoxia significantly upregulated HIF-1α protein. But the pretreatment with PX-478 for 20 hr under normoxia before 1-hr hypoxia attenuated the accumulation of HIF-1α induced by the 1-hr hypoxia. In PC3 cells, pretreatment with 20 μmol/L PX-478 before hypoxia inhibited HIF-1α by 40% compared to treatment with hypoxia alone. In DU 145 cells, pretreatment with 50 μmol/L PX-478 before hypoxia inhibited HIF-1α by 35% compared to treatment with hypoxia alone [1].

In nu/nu mice with C6 reporter xenografts, treatment with PX-478 at a dose of 30 mg/kg p.o. for 2 consecutive days prevented the transcriptional activity of HIF-1 in central ischemic regions of C6 tumors [2].

References:
[1].  Palayoor ST, Mitchell JB, Cerna D, et al. PX-478, an inhibitor of hypoxia-inducible factor-1α, enhances radiosensitivity of prostate carcinoma cells. International journal of cancer, 2008, 123(10): 2430-2437.
[2].  Schwartz DL, Powis G, Thitai-Kumar A, et al. The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Molecular cancer therapeutics, 2009, 8(4): 947-958.