2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK JAK/STAT Signaling PI3K/Akt/mTOR Apoptosis
  3. HSP EGFR Akt Survivin Apoptosis
  4. HVH-2930

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.

For research use only. We do not sell to patients.

HVH-2930

HVH-2930 Chemical Structure

CAS No. : 3034605-72-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

HVH-2930 Related Antibodies

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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.

HVH-2930 Related Antibodies

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 AUClast AUCinf Cmax Tmax T1/2 MRT0-inf CL Vd 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.
Molecular Weight

488.62

Formula

C29H36N4O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0466 mL 10.2329 mL 20.4658 mL
5 mM 0.4093 mL 2.0466 mL 4.0932 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HVH-29303034605-72-3HVH2930HVH 2930HSPEGFRAktSurvivinApoptosisHeat shock proteinsEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BHSP90 C-terminal domainHER2 signalingcancer stem cell-like propertiesJIMT-1BT474HEK293hERG channelsInhibitorinhibitorinhibit

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