PHY34
Based on 1 Customer Validation
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.43%
- CAS 番号: 2130033-55-3
- 分子式: C30H30O12
- 分子量:582.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
ATP6V0A2, cellular apoptosis susceptibility (CAS)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
0.043 μM
Compound: 114; PHY34
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Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability
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[PMID: 30830783] |
| OVCAR-3 | IC50 |
0.0042 μM
Compound: 114; PHY34
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Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability
Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability
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[PMID: 30830783] |
| OVCAR-8 | IC50 |
0.004 μM
Compound: 114; PHY34
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Antiproliferative activity against human OVCAR8 cells assessed as reduction in cell viability
Antiproliferative activity against human OVCAR8 cells assessed as reduction in cell viability
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[PMID: 30830783] |
PHY34 (0.001 nM-50 μM, 72 h) inhibits various cancer cells growth with nanomolar potency through activation of apoptosis based on enhanced cPARP levels and has the highest potency in HGSOC cell lines[1].
PHY34 (100 nM, 1 μM; 24 h) blocks the final breakdown of the autolysosomes in OVCAR8 at 100 nM, and in OVCAR3 at 1 μM, respectively[1].
PHY34 (10 nM, 24 h) inhibits the late-stage autophagy that precedes apoptosis induction in OVCAR8[1].
PHY34 (100 nM, 48 h) inhibits the late-stage autophagy that precedes apoptosis induction in OVCAR3[1].
PHY34 (0.01 nM-2 μM, 72 h) induces cell death in the presence of wild-type V0A2, but not V823I mutants in H4 cell[2].
PHY34 (10, 100 nM; 48 h, 72 h) changes subcellular localization of nuclear multiple proteins[2].
PHY34 (20 μM, 1 h) binds specificity with ATP6V0A2 subunit[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR8, OVCAR3, HT-29, MDA-MB-435, MDA-MB-231, IOSE80, FT33
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Concentration:0.001 nM-50 μM
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Incubation Time:72 h
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Result:Inhibited the growth of various cancer cells with IC50 values of 4 nM(OVCAR8, OVCAR3), 43.3 nM(HT-29) , 23 nM(MDA-MB-435) , 5.2 nM(MDA-MB-231).
Exhibited no toxicity to IOSE80 and FT33 (IC50 >50 μM).
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Cell Line:H4
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Concentration:0.01 nM-2 μM
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Incubation Time:72 h
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Result:Inhibited mutant cell with an IC50 value of 246 pM that was 1000-fold more potent than HTP-013(434 nM).
Conferred resistance in V8231 mutation and no impact activity in T216A mutation.
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Cell Line:OVCAR8, OVCAR3
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Concentration:10 nM, 100 nM
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Incubation Time:72 h
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Result:Increased the number of cells in early and late apoptosis in OVCAR8 and OVCAR3 at 10 nM and 100 nM, respectively.
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Cell Line:Hela
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Concentration:9.31 fM-20 μM
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Incubation Time:4 h
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Result:Sustained high levels of LC3B puncta with an EC50 value of 2 nM.
Inhibited autophagy with an EC50 value of 3.9 nM.
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Cell Line:OVCAR3
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Concentration:5 nM
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Incubation Time:4 h
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Result:Inhibited autophagy with an ED50 value of 6.29 nM, and was more potent than bafilomycin A1 (HY-100558) with an ED50 value of 29.1 nM.
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Cell Line:OVCAR8, OVCAR3, OVCAR4
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Concentration:10 nM, 100 nM
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Incubation Time:48 h, 72 h
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Result:Increased cPARP levels in OVCAR8 after 48 h at 10 nM, in OVCAR4 and OVCAR3 after 72 h at 100 nM, respectively.
Reversed the conversion of PARP to cPARP combined with RAP (HY-10219) of 1 μM.
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Cell Line:OVCAR8, OVCAR3, OVCAR4
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Concentration:10 nM
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Incubation Time:24 h, 48 h, 72 h
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Result:Promoted histone H3, LAMP1/2, ACSS2, and PCNA nuclear protein accumulation at 48 h.
Reduced expression of KPNA2 (Karyopherin subunit alpha 2) with time-dependent manner.
Increased nuclear accumulation of mutant p53 at 48 h.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OVCAR8-induced xenograft models in female nude mice[1].
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Dosage:0.75 mg/kg, three times a week for three weeks
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Administration:Intraperitoneal injection (i.p.)
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Result:Decreased tumor burden based on average abdominal radiant efficiency with no gross toxicity through analysis of fluorescence imaging.
化学情報
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CAS 番号 2130033-55-3
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性状 Solid
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分子量 582.55
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分子式 C30H30O12
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Color White to off-white
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SMILES
O=C1C2=C(C3=CC=C(OCO4)C4=C3)C5=CC(OC)=C(OC)C=C5C(O[C@H]6[C@@H]([C@]7([H])[C@](OC(C)(O7)C)([H])[C@H](O6)CO)O)=C2CO1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (171.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (290 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7166 mL | 8.5830 mL | 17.1659 mL | 42.9148 mL |
| 5 mM | 0.3433 mL | 1.7166 mL | 3.4332 mL | 8.5830 mL | |
| 10 mM | 0.1717 mL | 0.8583 mL | 1.7166 mL | 4.2915 mL | |
| 15 mM | 0.1144 mL | 0.5722 mL | 1.1444 mL | 2.8610 mL | |
| 20 mM | 0.0858 mL | 0.4291 mL | 0.8583 mL | 2.1457 mL | |
| 25 mM | 0.0687 mL | 0.3433 mL | 0.6866 mL | 1.7166 mL | |
| 30 mM | 0.0572 mL | 0.2861 mL | 0.5722 mL | 1.4305 mL | |
| 40 mM | 0.0429 mL | 0.2146 mL | 0.4291 mL | 1.0729 mL | |
| 50 mM | 0.0343 mL | 0.1717 mL | 0.3433 mL | 0.8583 mL | |
| 60 mM | 0.0286 mL | 0.1430 mL | 0.2861 mL | 0.7152 mL | |
| 80 mM | 0.0215 mL | 0.1073 mL | 0.2146 mL | 0.5364 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1717 mL | 0.4291 mL |
PHY34 関連分類
HY-122650 関連分類
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