Cat. No.: HY-B1305

Chloropyramine hydrochloride

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Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.

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

Purity: 99.64%
CAS No.: 6170-42-9
Formula: C₁₆H₂₁Cl₂N₃
Molecular Weight:326.26

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Chloropyramine hydrochloride Chemical Structure

CAS No.: 6170-42-9

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.

IC₅₀ & Target^[1]

H₁ Receptor

VEGFR-3

All Histamine Receptor Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1 μM Compound: 1	Cytotoxicity against human A375 cells after 72 hrs by MTS assay Cytotoxicity against human A375 cells after 72 hrs by MTS assay	[PMID: 19610651]
BT-474	IC₅₀	1 μM Compound: 1	Cytotoxicity against human BT474 cells after 72 hrs by MTS assay Cytotoxicity against human BT474 cells after 72 hrs by MTS assay	[PMID: 19610651]
COLO 205	IC₅₀	1 μM Compound: 1	Cytotoxicity against human COLO205 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against human COLO205 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 19610651]
HT-29	IC₅₀	1 μM Compound: 1	Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 19610651]
MDA-MB-231	IC₅₀	1 μM Compound: 1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTS assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTS assay	[PMID: 19610651]
MIA PaCa-2	IC₅₀	1 μM Compound: 1	Cytotoxicity against human MIAPaCa2 cells after 72 hrs by MTS assay Cytotoxicity against human MIAPaCa2 cells after 72 hrs by MTS assay	[PMID: 19610651]
PANC-1	IC₅₀	1 μM Compound: 1	Cytotoxicity against human PANC1 cells after 72 hrs by MTS assay Cytotoxicity against human PANC1 cells after 72 hrs by MTS assay	[PMID: 19610651]
SAOS-2	IC₅₀	1 μM Compound: 1	Cytotoxicity against human Saos2 cells after 72 hrs by MTS assay Cytotoxicity against human Saos2 cells after 72 hrs by MTS assay	[PMID: 19610651]
T47D	IC₅₀	1 μM Compound: 1	Cytotoxicity against human T47D cells after 72 hrs by MTS assay Cytotoxicity against human T47D cells after 72 hrs by MTS assay	[PMID: 19610651]

In Vitro

BT474 cells are highly sensitive to Chloropyramine hydrochloride (compound 1) treatment, whereby 1 µM concentrations cause a 40% reduction of viability after 48 h of treatment. It is found that at 1 µM concentrations of Chloropyramine hydrochloride, viability of control MCF7-pcDNA3 cells is significantly higher than the viability of MCF7-VEGFR-3 cells (P<0.01) and at 10 µM concentration this difference reaches twofold (P<0.001). In the BT474 cells treatment with Chloropyramine hydrochloride also leads to a concentration-dependent decrease of cell proliferation. When treatment with Chloropyramine hydrochloride is continued for 48 h, the breast cancer cells that overexpressed VEGFR-3 undergo apoptosis. This effect is dose-dependent, with 10 µM Chloropyramine hydrochloride inducing apoptosis in more than 60% of BT474 cells. In our model cell lines MCF7-pcDNA3 and MCF7-VEGFR-3, treatment with 10 µM Chloropyramine hydrochloride for 48 h leads to a 4-fold increase in apoptotic cell death in the cell line that overexpressed VEGFR-3 (18% versus 76 % respectively)^[1].

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

In Vivo

Chloropyramine hydrochloride causes a dramatic reduction of tumor growth in both model systems whereby the tumor size in the treated groups is approximately 20% of the tumor size in vehicle control groups. Doxorubicin administered at 3 mg/kg causes approximately 60% reduction of tumor growth, but has no effect on tumor growth at 0, 3 mg/kg. In contrast, there is a modest effect of Chloropyramine hydrochloride alone (50% reduction of tumor growth). The low-dose combination of Chloropyramine hydrochloride and doxorubicin has a prolonged anti-tumor effect (85% reduction of tumor growth) that is greater than either drug alone^[1].

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

Chemical Information

CAS No. 6170-42-9
Appearance Solid
Molecular Weight 326.26
Formula C₁₆H₂₁Cl₂N₃
Color White to off-white
SMILES

CN(C)CCN(CC1=CC=C(Cl)C=C1)C2=NC=CC=C2.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (306.50 mM; Need ultrasonic)

DMSO : 30 mg/mL (91.95 mM; Need ultrasonic and warming; 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

3.0650 mL

15.3252 mL

30.6504 mL

5 mM

0.6130 mL

3.0650 mL

6.1301 mL

10 mM

0.3065 mL

1.5325 mL

3.0650 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 50 mg/mL (153.25 mM); Clear solution; Need ultrasonic

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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Protocol

Kinase Assay^[1]

Cells are incubated in presence or absence of Chloropyramine hydrochloride and stained with anti-FAK antibody 4.47 or in combination with paxillin or VEGFR-3. Detection is done with Alexa Fluor 546 secondary antibody and for dual staining combination of Alexa Fluor 488 and Alexa Fluor 546 secondary antibody is used^[1].

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

Cell Assay^[1]

Cell survival is assayed in MTS assay by measuring mitochondrial dehydrogenase activity of metabolically active cells. 5.0×10³ (100 µL) cells are plated in 96-well plates and are allowed to attach overnight. One hundred microliters of fresh media with or without Chloropyramine hydrochloride is added to each well. Cells are treated for designated amount of time. MTS assay is performed according the manufacturers protocol^[1].

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

Animal Administration^[1]

BT474 and MCF7-VEGFR-3 cells at a concentration of 2 to 5×10⁶ cells per 200 µL are subcutaneously injected into the right flank of the 5 to 6 week old mice, 5 in each group. Treatment with Chloropyramine hydrochloride is started next day after cells injection via intraperitoneal injection (IP) once a day. Tumor size is measured thrice weekly and volume is calculated using the formula length×width²×0.5. Animals are sacrificed after 21 days of treatment or when tumor size reaches protocol end point. Tumor is excised, measured and preserved for protein and RNA preparation and cytochemistry^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

References

[1]. Kurenova EV, et al. Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo. J Med Chem. 2009 Aug 13;52(15):4716-24. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	3.0650 mL	15.3252 mL	30.6504 mL	76.6260 mL
	5 mM	0.6130 mL	3.0650 mL	6.1301 mL	15.3252 mL
	10 mM	0.3065 mL	1.5325 mL	3.0650 mL	7.6626 mL
	15 mM	0.2043 mL	1.0217 mL	2.0434 mL	5.1084 mL
	20 mM	0.1533 mL	0.7663 mL	1.5325 mL	3.8313 mL
	25 mM	0.1226 mL	0.6130 mL	1.2260 mL	3.0650 mL
	30 mM	0.1022 mL	0.5108 mL	1.0217 mL	2.5542 mL
	40 mM	0.0766 mL	0.3831 mL	0.7663 mL	1.9157 mL
	50 mM	0.0613 mL	0.3065 mL	0.6130 mL	1.5325 mL
	60 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2771 mL
	80 mM	0.0383 mL	0.1916 mL	0.3831 mL	0.9578 mL
H₂O	100 mM	0.0307 mL	0.1533 mL	0.3065 mL	0.7663 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Chloropyramine hydrochloride

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All Histamine Receptor Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Chloropyramine hydrochloride Related Classifications

HY-B1305 Related Classifications