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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder (seal) | ||||||||
化学式 | C13H20Cl4N2O3 |
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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) |
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* <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. |
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. |
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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] |
細胞アッセイ | 細胞株 | NPC cell lines |
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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 |
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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. |
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]
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 |
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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