[CAS NO. 6170-42-9] Chloropyramine hydrochloride
PRODUCTS SPECIFICATIONS [6170-42-9]
DESCRIPTION [6170-42-9]
Overview
| MDL | MFCD00079009 |
|---|---|
| Molecular Weight | 326.26 |
| Molecular Formula | C16H21Cl2N3 |
| SMILES | CN(C)CCN(CC1=CC=C(Cl)C=C1)C2=NC=CC=C2.[H]Cl |
Summary
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK .
IC50 & Target
|
H 1 Receptor |
VEGFR-3 |
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] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
H 2 O : 100 mg/mL ( 306.50 mM ; Need ultrasonic)
DMSO : 30 mg/mL ( 91.95 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
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1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (153.25 mM); Clear solution; Need ultrasonic
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2.
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3.
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
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.38 mM); Clear solution
Synonyms