Art. -Nr.: HY-161781

HVH-2930

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HVH-2930 is a HSP90 C-terminal domain inhibitor with high oral bioavailability. HVH-2930 downregulates HSP90 client proteins, inhibits the HER2 signaling pathway, induces apoptosis, and suppresses the proliferation of breast cancer cells. HVH-2930 inhibits the proliferation of tumors sensitive or resistant to Trastuzumab (HY-P9907). HVH-2930 is applicable to relevant research on breast cancer.

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Reinheit: 96.54%
CAS. Nr.: 3034605-72-3
Formel: C₂₉H₃₆N₄O₃
Molecular Weight:488.62

Speicherung:

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

HVH-2930 Chemical Structure

CAS. Nr.: 3034605-72-3

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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

Biologische Aktivität

Beschreibung

Alle HSP Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-474	IC₅₀	6.86 μM Compound: 12d	Antiproliferative activity against human Trastuzumab-sensitive BT474 cell assessed as inhibition of cell viability measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human Trastuzumab-sensitive BT474 cell assessed as inhibition of cell viability measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 38971048]

In Vitro

HVH-2930 (0.1-20 μM; 72 h) inhibits the viability of Trastuzumab (HY-P9907)-sensitive BT474 human breast cancer cells (IC₅₀ = 6.86 μM) and drug-resistant JIMT-1 human breast cancer cells (IC₅₀ = 4.42 μM), and exhibits only extremely low cytotoxicity in normal HEK293 cells after 72 h of treatment^[1].
HVH-2930 (10 μM; 48-72 h) downregulates the expression and activation of major HSP90 client proteins in Trastuzumab-sensitive BT474 and trastuzumab-resistant JIMT-1 human breast cancer cells in a time-dependent manner^[1].
HVH-2930 (0-30 μM) inhibits hERG channel currents in a concentration-dependent manner in CHO cells expressing hERG, with an inhibition rate of 57% at 10 μM in fluorescence polarization assays^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

trastuzumab-sensitive BT474 human breast cancer cells, trastuzumab-resistant JIMT-1 human breast cancer cells
Concentration:

10 μM
Incubation Time:

48 h, 72 h
Result:

Downregulated total HER2 and AKT protein levels in a time-dependent manner in both cell lines.
Reduced phosphorylation of HER2 (Tyr1221/1222) and AKT (Ser473) in a time-dependent manner in both cell lines.
Downregulated HSP90 client proteins cyclin D1 and survivin in both cell lines.

Parmacokinetics

Species	Dose	Route	AUC_last	AUC_inf	C_max	T_max	T_1/2	MRT_0-inf	CL	V_d	Bioavailability	C₀
Rat^[1]	5 mg/kg	i.v.	771 ng·h/mL	1059 ng·h/mL	/	/	4.4 h	5.4 h	84.5 mL/min	31.2 L/kg	/	342 ng/mL
Rat^[1]	10 mg/kg	p.o.	1032 ng·h/mL	2957 ng·h/mL	159 ng/mL	4.0 h	9.6 h	15.0 h	47.3 mL/min	3.6 L/kg	66.9 %	/

In Vivo

HVH-2930 (20 mg/kg; i.p.; every other day; 40 days) significantly reduces tumor burden in a trastuzumab-resistant HER2-positive breast cancer xenograft model without causing substantial weight loss^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (female, 6 weeks old, orthotopic xenograft via injection of trastuzumab-resistant JIMT-1 cells)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; every other day; 40 days
Result:

Considerably inhibited JIMT-1 tumor growth.
Reduced tumor volume and weight compared to vehicle controls.
Caused no substantial decline in body weight.

Chemical Information

CAS. Nr. 3034605-72-3
Appearance Solid
Molecular Weight 488.62
Formel C₂₉H₃₆N₄O₃
Color Light yellow to yellow
SMILES

O=C(C1=C(OC)C(C=CC(C)(C)O2)=C2C=C1)NC3=CC4=C(C=C3)C(C)=NN4CCC5CCN(C)CC5
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 (204.66 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

2.0466 mL

10.2329 mL

20.4658 mL

5 mM

0.4093 mL

2.0466 mL

4.0932 mL

10 mM

0.2047 mL

1.0233 mL

2.0466 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.12 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.12 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 (275 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. La MT, et al. Discovery of indazole inhibitors for heat shock protein 90 as anti-cancer agents. Eur J Med Chem. 2024;276:116620. [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	2.0466 mL	10.2329 mL	20.4658 mL	51.1645 mL
	5 mM	0.4093 mL	2.0466 mL	4.0932 mL	10.2329 mL
	10 mM	0.2047 mL	1.0233 mL	2.0466 mL	5.1165 mL
	15 mM	0.1364 mL	0.6822 mL	1.3644 mL	3.4110 mL
	20 mM	0.1023 mL	0.5116 mL	1.0233 mL	2.5582 mL
	25 mM	0.0819 mL	0.4093 mL	0.8186 mL	2.0466 mL
	30 mM	0.0682 mL	0.3411 mL	0.6822 mL	1.7055 mL
	40 mM	0.0512 mL	0.2558 mL	0.5116 mL	1.2791 mL
	50 mM	0.0409 mL	0.2047 mL	0.4093 mL	1.0233 mL
	60 mM	0.0341 mL	0.1705 mL	0.3411 mL	0.8527 mL
	80 mM	0.0256 mL	0.1279 mL	0.2558 mL	0.6396 mL
	100 mM	0.0205 mL	0.1023 mL	0.2047 mL	0.5116 mL

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HVH-2930

Anti-Infection Compound Library

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Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle HSP Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HVH-2930 Related Classifications

HY-161781 Related Classifications