PX-478 2HCl

製品コードS7612 バッチS761205

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)
* <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 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] PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. ^[3]
in vivo	In HT-29 human colon cancer xenografts, PX-478 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, PX-478 (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, PX-478 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 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]

PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. ^[3]

in vivo

In HT-29 human colon cancer xenografts, PX-478 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, PX-478 (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, PX-478 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
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

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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：

PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 4(10):1508-1525]	PubMed: 37723306
AMPK-HIF-1α signaling enhances glucose-derived de novo serine biosynthesis to promote glioblastoma growth [ J Exp Clin Cancer Res, 2023, 42(1):340]	PubMed: 38098117
Hypoxia-inducible factor 1A inhibition overcomes castration resistance of prostate tumors [ EMBO Mol Med, 2023, e17209.]	PubMed: 37070472
Hypoxia-inducible factor 1α modulates interstitial pneumonia-mediated lung cancer progression [ J Transl Med, 2023, 21(1):857]	PubMed: 38012636
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.07.012]	PubMed: 37562653
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 16(5):823-846]	PubMed: 37562653
Withaferin A Increases the Effectiveness of Immune Checkpoint Blocker for the Treatment of Non-Small Cell Lung Cancer [ Cancers (Basel), 2023, 15(12)3089]	PubMed: 37370701
Disruption of sirtuin 7 in zebrafish facilitates hypoxia tolerance [ J Biol Chem, 2023, 299(8):105074]	PubMed: 37481210
Hypoxia-inducible factor 1α inhibitor induces cell death via suppression of BCR-ABL1 and Met expression in BCR-ABL1 tyrosine kinase inhibitor sensitive and resistant chronic myeloid leukemia cells [ BMB Rep, 2023, 56(2):78-83]	PubMed: 36195570
Glycolytic reprogramming is involved in tissue remodeling on chronic rhinosinusitis [ PLoS One, 2023, 18(2):e0281640]	PubMed: 36795696

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