| Identification | Back Directory | [Name]
PHY34 | [CAS]
2130033-55-3 | [Synonyms]
PHY34
Naphtho[2,3-c]furan-1(3H)-one, 9-(1,3-benzodioxol-5-yl)-6,7-dimethoxy-4-[[3,4-O-(1-methylethylidene)-β-D-galactopyranosyl]oxy]- | [Molecular Formula]
C30H30O12 | [MOL File]
2130033-55-3.mol | [Molecular Weight]
582.56 |
| Chemical Properties | Back Directory | [Boiling point ]
841.4±65.0 °C(Predicted) | [density ]
1.412±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 10 mg/ml | [form ]
A solid | [pka]
12.43±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
PMJUVXNBXQVOOP-VITQGGQRNA-N | [SMILES]
O=C1OCC2=C(O[C@@H]3O[C@H](CO)[C@]4([H])OC(C)(C)O[C@]4([H])[C@H]3O)C3=CC(OC)=C(OC)C=C3C(C3=CC=C4OCOC4=C3)=C12 |&1:7,9,12,19,21,r| |
| Hazard Information | Back Directory | [Uses]
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer[1][2]. | [in vivo]
PHY34 (0.75 mg/kg, i.p., 3 times a week for 3 weeks) inhibits tumor growth and reduces Ki67 expression in tumor tissue in a female nude mouse tumor bearing model constructed by OVCAR8[1].
PHY34 Pharmacokinetics[1]
| Parameter | Units | IV | IP | PO | | Dose | mg/kg | 0.6 | 1.8 | 75 | | Dose | nmol | 1029.9 | 3089.8 | 128742.1 | | T1/2 | hr | 6.2 | 8.4 | 12.3 | | Tmax | hr | 0.08 | 0.25 | 0.25 | | Cmax | nmol/L | 288.8 | 519.5 | 323.6 | | AUClast | hr*nmol/L | 198.8 | 360.5 | 599.9 | | AUCinf | hr*nmol/L | 215.8 | 366.5 | 663.3 | | Vz | L/kg | 42.7 | 101.6 | 3430.3 | | CI | L/hr/kg | 4.8 | 8.4 | 194.1 | | MRT | hr | 6.1 | 1.9 | 7.8 | | F* | % | - | 56.6 | 2.5 |
| Animal Model: | OVCAR8-induced xenograft models in female nude mice[1]. | | Dosage: | 0.75 mg/kg, three times a week for three weeks | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Decreased tumor burden based on average abdominal radiant efficiency with no gross toxicity through analysis of fluorescence imaging. |
| [References]
[1] Young AN,et al. Phyllanthusmin Derivatives Induce Apoptosis and Reduce Tumor Burden in High-Grade Serous Ovarian Cancer by Late-Stage Autophagy Inhibition. Mol Cancer Ther. 2018 Oct;17(10):2123-2135. DOI:10.1158/1535-7163.MCT-17-1195
[2] Salvi A, et al. PHY34 inhibits autophagy through V-ATPase V0A2 subunit inhibition and CAS/CSE1L nuclear cargo trafficking in high grade serous ovarian cancer. Cell Death Dis. 2022 Jan 10;13(1):45. DOI:10.1038/s41419-021-04495-w |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
|