Art. -Nr.: HY-122650

PHY34

Name: PHY34
Brand: MedChemExpress
SKU: HY-122650
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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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Reinheit: 98.43%
CAS. Nr.: 2130033-55-3
Formel: C₃₀H₃₀O₁₂
Molecular Weight:582.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PHY34 Chemical Structure

CAS. Nr.: 2130033-55-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

ATP6V0A2, cellular apoptosis susceptibility (CAS)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	0.043 μM Compound: 114; PHY34	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	[PMID: 30830783]
OVCAR-3	IC₅₀	0.0042 μM Compound: 114; PHY34	Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability	[PMID: 30830783]
OVCAR-8	IC₅₀	0.004 μM Compound: 114; PHY34	Antiproliferative activity against human OVCAR8 cells assessed as reduction in cell viability Antiproliferative activity against human OVCAR8 cells assessed as reduction in cell viability	[PMID: 30830783]

In Vitro

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.

Cell Viability Assay^[1]^[2]

Cell Line:

OVCAR8, OVCAR3, HT-29, MDA-MB-435, MDA-MB-231, IOSE80, FT33
Concentration:

0.001 nM-50 μM
Incubation Time:

72 h
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).

Cell Viability Assay^[2]

Cell Line:

H4
Concentration:

0.01 nM-2 μM
Incubation Time:

72 h
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.

Apoptosis Analysis^[1]

Cell Line:

OVCAR8, OVCAR3
Concentration:

10 nM, 100 nM
Incubation Time:

72 h
Result:

Increased the number of cells in early and late apoptosis in OVCAR8 and OVCAR3 at 10 nM and 100 nM, respectively.

Cell Autophagy Assay^[1]

Cell Line:

Hela
Concentration:

9.31 fM-20 μM
Incubation Time:

4 h
Result:

Sustained high levels of LC3B puncta with an EC₅₀ value of 2 nM.
Inhibited autophagy with an EC₅₀ value of 3.9 nM.

Cell Autophagy Assay^[2]

Cell Line:

OVCAR3
Concentration:

5 nM
Incubation Time:

4 h
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.

Western Blot Analysis^[1]^[2]

Cell Line:

OVCAR8, OVCAR3, OVCAR4
Concentration:

10 nM, 100 nM
Incubation Time:

48 h, 72 h
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.

Western Blot Analysis^[2]

Cell Line:

OVCAR8, OVCAR3, OVCAR4
Concentration:

10 nM
Incubation Time:

24 h, 48 h, 72 h
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.

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
T_1/2	hr	6.2	8.4	12.3
T_max	hr	0.08	0.25	0.25
C_max	nmol/L	288.8	519.5	323.6
AUC_last	hr^*nmol/L	198.8	360.5	599.9
AUC_inf	hr^*nmol/L	215.8	366.5	663.3
V_z	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.

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.

Chemical Information

CAS. Nr. 2130033-55-3
Appearance Solid
Molecular Weight 582.55
Formel C₃₀H₃₀O₁₂
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7166 mL

8.5830 mL

17.1659 mL

5 mM

0.3433 mL

1.7166 mL

3.4332 mL

10 mM

0.1717 mL

0.8583 mL

1.7166 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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PHY34

3BDO

Chloroquine phosphate

Autophinib

SBI-0206965

EN6

ROC-325

Nortriptyline hydrochloride

SMER28

QX77

Chloroquine phosphate (Standard)

STF-62247

Nortriptyline hydrochloride (Standard)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

PHY34

3BDO

Chloroquine phosphate

Autophinib

SBI-0206965

EN6

ROC-325

Nortriptyline hydrochloride

SMER28

QX77

Chloroquine phosphate (Standard)

STF-62247

Nortriptyline hydrochloride (Standard)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PHY34 Related Classifications

HY-122650 Related Classifications

Bioz