PX-478 2HCl

製品コードS7612 バッチS761206

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder (seal)

化学式

C₁₃H₂₀Cl₄N₂O₃

分子量

394.12

CAS No.

685898-44-6

Solubility (25°C)*

体外

DMSO

79 mg/mL (200.44 mM)

Water

79 mg/mL (200.44 mM)

Ethanol

79 mg/mL (200.44 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
in vitro	PX-478 2HCl lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. ^[2] This compound also enhances the radiosensitivity of prostate carcinoma PC3 cells. ^[3]
in vivo	In HT-29 human colon cancer xenografts, PX-478 2HCl suppresses HIF-1alpha levels and inhibits the expression of HIF-1 target genes including vascular endothelial growth factor and the glucose transporter-1. In addition, this compound (100 or 120 mg/kg i.p.) also shows antitumor activity including cures against several established human tumor xenografts that is related to the levels of HIF-1α. ^[1] In high-fat-diet mice, this chemical causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. ^[4]

製品説明

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.

in vitro

PX-478 2HCl lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. ^[2]

This compound also enhances the radiosensitivity of prostate carcinoma PC3 cells. ^[3]

in vivo

In HT-29 human colon cancer xenografts, PX-478 2HCl suppresses HIF-1alpha levels and inhibits the expression of HIF-1 target genes including vascular endothelial growth factor and the glucose transporter-1. In addition, this compound (100 or 120 mg/kg i.p.) also shows antitumor activity including cures against several established human tumor xenografts that is related to the levels of HIF-1α. ^[1]

In high-fat-diet mice, this chemical causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NPC cell lines
	濃度	10 μM
	反応時間	24 h
	実験の流れ	Cells were treated with 10 or 50 μM PX-478 2HCl.
動物実験	動物モデル	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.
	投薬量	100 or 120 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/15026543/
https://pubmed.ncbi.nlm.nih.gov/18202012/
https://pubmed.ncbi.nlm.nih.gov/18729192/

https://pubmed.ncbi.nlm.nih.gov/23249949/
https://pubmed.ncbi.nlm.nih.gov/30479336/

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カスタマーフィードバック

: Data from [Data independently produced by , , Theranostics, 2018, 8(15):4050-4061]

: Data from [Data independently produced by , , Free Radic Biol Med, 2018, 130:278-287]

: Data from [Data independently produced by , , Br J Pharmacol, 2017, 174(5):409-423]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Lactate-HIF-1a axis promotes PINK1-dependent mitophagy to protect porcine granulosa cells against hypoxic stress [ Int J Biol Macromol, 2025, 332(Pt 1):148503]	PubMed: 41138862
HIF1A-mediated pathways promote euploid cell survival in chromosomally mosaic embryos [ Elife, 2025, 13RP101912]	PubMed: 41086100
Rapamycin Increases the Development Competence of Yak (Bos grunniens) Oocytes by Promoting Autophagy via Upregulating 17β-Estradiol and HIF-1α During In Vitro Maturation [ Animals (Basel), 2025, 15(3)365]	PubMed: 39943135
Oxygen enhances antiviral innate immunity through maintenance of EGLN1-catalyzed proline hydroxylation of IRF3 [ Nat Commun, 2024, 15(1):3533]	PubMed: 38670937
Wild-type IDH2 is a therapeutic target for triple-negative breast cancer [ Nat Commun, 2024, 15(1):3445]	PubMed: 38658533
Single-embryo transcriptomic atlas of oxygen response reveals the critical role of HIF-1α in prompting embryonic zygotic genome activation [ Redox Biol, 2024, 72:103147]	PubMed: 38593632
Spring viremia of carp virus infection induces hypoxia response in zebrafish by stabilizing hif1α [ J Virol, 2024, e0149124.]	PubMed: 39601573
Integrin α6β4 Upregulates PTPRZ1 Through UCHL1-Mediated Hif-1α Nuclear Accumulation to Promote Triple-Negative Breast Cancer Cell Invasive Properties [ Cancers (Basel), 2024, 16(21)3683]	PubMed: 39518121
Lactate Promotes Hypoxic Granulosa Cells' Autophagy by Activating the HIF-1α/BNIP3/Beclin-1 Signaling Axis [ Genes (Basel), 2024, 16(1)14]	PubMed: 39858561
HIF1A contributes to the survival of aneuploid and mosaic pre-implantation embryos [ bioRxiv, 2024, 2023.09.04.556218]	PubMed: 39071426

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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