| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Fendiline targets multiple molecular targets including L-type calcium channels, α2-adrenergic receptors, and K-Ras. It inhibits K-Ras plasma membrane localization, blocking the proliferation of cancer cell lines expressing oncogenic mutant K-Ras. As a STING agonist, it activates the STING pathway, leading to antitumor immune responses. The compound also blocks calcium channels, contributing to its antianginal effects.
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| ln Vitro |
In vitro, Fendiline hydrochloride inhibits K-Ras plasma membrane localization with an IC50 of 9.64 μM. It blocks proliferation of cancer cell lines expressing oncogenic mutant K-Ras. The compound demonstrates potency in inhibiting dual action probes in a Huntington cell model, inducing genomic imprint erasure, and enhancing SMN2 splice variant expression. It modulates miRNAs and exhibits bioactivity across various assays.
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| ln Vivo |
In vivo, Fendiline hydrochloride is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26, and B16F10). As a STING agonist, it activates antitumor immune responses, leading to tumor growth inhibition. The compound has been studied in animal models of cancer for its efficacy as a single agent or in combination with other immunotherapies. It is also used as an antianginal agent for the treatment of coronary heart disease.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for calcium channel blockers typically use radioligand binding with [³H]nitrendipine or [³H]PN200-110 for L-type calcium channels. Membranes prepared from cardiac or smooth muscle tissue are incubated with the radioligand and varying concentrations of Fendiline. Specific binding is determined by subtracting non-specific binding (defined by excess nifedipine). Ki values are calculated from competition curves. For K-Ras inhibition, assays measure the effect of the compound on K-Ras membrane localization using cell fractionation and Western blotting.
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| Cell Assay |
Cellular assays for Fendiline typically use cancer cell lines expressing oncogenic mutant K-Ras (e.g., pancreatic, colorectal, or lung cancer cells). Cells are treated with varying concentrations of Fendiline, and cell proliferation is measured using MTT, CCK-8, or colony formation assays. K-Ras membrane localization is assessed by cell fractionation followed by Western blotting. STING activation is measured by assessing downstream signaling (e.g., phosphorylation of TBK1 and IRF3) and cytokine production (e.g., IFN-β).
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| Animal Protocol |
In vivo animal studies for antitumor efficacy typically use syngeneic mouse tumor models (e.g., MC38, CT26, B16F10). Mice are implanted with tumor cells and treated with Fendiline hydrochloride administered intraperitoneally or orally at various doses. Tumor growth is measured by caliper, and tumor weight is determined at study termination. Immune cell infiltration and activation are assessed by flow cytometry and immunohistochemistry. Survival is monitored as an endpoint. Combination studies with immune checkpoint inhibitors may also be performed.
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| ADME/Pharmacokinetics |
Fendiline hydrochloride is orally bioavailable with good absorption following oral administration. As a lipophilic small molecule, it distributes to tissues including the heart (for antianginal effects) and tumors (for anticancer effects). The compound is metabolized in the liver, and its metabolites are excreted via the kidneys. Detailed PK parameters such as half-life, Cmax, and AUC are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of Fendiline hydrochloride would typically include acute and repeated-dose toxicity in rodents and dogs, as well as genotoxicity and safety pharmacology assessments. The compound is generally well-tolerated at therapeutic doses. Common side effects may include hypotension, bradycardia, and gastrointestinal disturbances, which are related to its calcium channel-blocking activity. Serious adverse effects are rare. The compound has a long history of use as an antianginal agent.
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| Additional Infomation |
It is a coronary vasodilator; it inhibits calcium function in the excitation-contraction coupling of muscle cells; and it is considered an antiarrhythmic and antianginal drug.
Fendiline hydrochloride is a multi-target compound with antianginal, anticancer, and immunomodulatory activities. It inhibits K-Ras plasma membrane localization (IC50 = 9.64 μM), blocks L-type calcium channels, antagonizes α2-adrenergic receptors, and activates STING. The compound inhibits the growth of refractory cold tumors (MC38, CT26, B16F10) and is used as an antianginal agent for coronary heart disease. It is available for research use and has been studied in various pharmacological contexts. |
| Molecular Formula |
C23H26CLN
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|---|---|
| Molecular Weight |
351.91
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| Exact Mass |
351.175
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| CAS # |
13636-18-5
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| PubChem CID |
5702162
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| Appearance |
White to off-white solid powder
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| Density |
1.031g/cm3
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| Boiling Point |
452.1ºC at 760mmHg
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| Flash Point |
207.9ºC
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| Vapour Pressure |
2.3E-08mmHg at 25°C
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| LogP |
6.752
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
303
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NJXWZWXCHBNOOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N.ClH/c1-19(20-11-5-2-6-12-20)24-18-17-23(21-13-7-3-8-14-21)22-15-9-4-10-16-22;/h2-16,19,23-24H,17-18H2,1H3;1H
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| Chemical Name |
3,3-diphenyl-N-(1-phenylethyl)propan-1-amine;hydrochloride
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| Synonyms |
Fendiline HCl; Fendiline Hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~85.25 mM)
H2O : ~1.82 mg/mL (~5.17 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8416 mL | 14.2082 mL | 28.4164 mL | |
| 5 mM | 0.5683 mL | 2.8416 mL | 5.6833 mL | |
| 10 mM | 0.2842 mL | 1.4208 mL | 2.8416 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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