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PX-478 HCl

HIF-1alpha inhibitor

PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity.

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Biological Activity

Target & Activity

Target	Activity	Value
HIF-1α

Cellular Effect

Cell Line	Activity	Value	Description	Reference
MCF7	IC50	19.7 μM	Antiproliferative activity against human MCF7 cells after 72 hrs under hypoxic condition by MTT assay	[PMID: 28209257]
MDA-MB-231	IC50	62.8 μM	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs under hypoxic condition by MTT assay	[PMID: 28209257]
MDA-MB-468	IC50	45.1 μM	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs under hypoxic condition by MTT assay	[PMID: 28209257]

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	685898-44-6
Applications	HIF-1alpha inhibitor
Formula	C₁₃H₂₀Cl₄N₂O₃
Molecular Weight	394.12
SMILES	C1=CC(=CC=C1C[C@@H](C(=O)O)N)[N+](CCCl)(CCCl)[O-].Cl.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	73 mg/mL (185.21 mM)
Water	73 mg/mL (185.21 mM)
Ethanol	73 mg/mL (185.21 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.