| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
CD437 is a selective agonist of retinoic acid receptor gamma (RARγ). It binds to RARγ with high affinity (Kd = 77 nM) and is selective over RARα (Kd = 6.5 µM) and RARβ (Kd = 2.5 µM). By activating RARγ, CD437 modulates the transcription of target genes involved in cell growth, differentiation, and apoptosis.
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| ln Vitro |
CD437 is a specific agonist of RARγ. After treating these lung cancer cell lines with 10 μM CD437 for two days, the growth inhibitory impact of CD437 was visible. The number of H460, SK-MES-1, A549, and H292 cells was shown to be decreased by CD437 in dose-response assays; its 50% inhibition values were roughly 0.5, 0.4, 3 and 0.85 μM, respectively [1]. All melanoma cell lines showed significant dose-dependent growth suppression following a 72-hour treatment with CD437. After three days, only around 5% to 25% of cells were still present at a concentration of 5 μM CD437. The greatest variation was found in the CD437 concentrations needed for 50% growth inhibition (IC50), which varied from 10 μM for MeWo to 0.1 μM for SK-Mel-23 [2].
CD437 exhibits potent in vitro antiproliferative activity and induces apoptosis in various cancer cell lines. In lung cancer cell lines, it shows growth inhibition with IC50 values of approximately 0.5 μM (H460), 0.4 μM (SK-MES-1), 3 μM (A549), and 0.85 μM (H292) after two days of treatment. The compound induces cell cycle arrest and apoptosis. Its effects are mediated through RARγ activation and AP-1 signaling. |
| ln Vivo |
CD437 therapy halted the growth of the tumor within these tumors; the impact was maintained for more than three weeks after therapy was ceased, and it reached statistical significance (P<0.01) on day 13, three days after CD437 was initially administered. Subsequent histological examination revealed that c-fos mRNA levels were considerable along the tumor's basal border in tumors treated with CD437 [2].
Specific in vivo activity data for CD437 is not extensively detailed in the available literature. As a potent inducer of apoptosis and inhibitor of tumor growth in vitro, it has been investigated for its potential anticancer effects in vivo. Studies would typically involve administration to tumor-bearing animals to evaluate its efficacy and pharmacokinetic properties. |
| Enzyme Assay |
CD437's activity as an RARγ agonist is assessed using in vitro receptor binding assays to measure its affinity for RARγ, RARα, and RARβ. These assays determine the compound's selectivity for RARγ over other RAR subtypes. Functional assays, such as reporter gene assays, can be used to measure RARγ-mediated transcriptional activity.
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| Cell Assay |
Cellular assays for CD437 involve treating cancer cell lines with the compound and measuring cell viability, proliferation, and apoptosis. Cell viability is assessed using MTT or other cell viability assays. Apoptosis is evaluated by measuring caspase activation, PARP cleavage, or using annexin V staining. The compound's effects on cell cycle progression are also assessed.
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| Animal Protocol |
In vivo animal model protocols for CD437 would involve its administration to tumor-bearing mice to evaluate its antitumor efficacy. The compound is typically administered systemically (e.g., orally or intraperitoneally). Tumor growth inhibition, apoptosis induction in tumor tissues, and pharmacokinetic parameters would be assessed.
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| ADME/Pharmacokinetics |
CD437 has a molecular weight of 398.49 and a molecular formula of C27H26O3. It is supplied as a solid and should be stored at -20°C. The compound is soluble in DMSO. Its lipophilic nature suggests good cell permeability. Specific pharmacokinetic data is not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
CD437 is intended for research use only and not for human consumption. As a research compound, its comprehensive toxicological profile may not be fully characterized. Standard safety assessments would be required for clinical development. The compound is generally handled with standard laboratory safety precautions.
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| References |
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| Additional Infomation |
CD437 is a naphthoic acid, specifically 6-phenylnaphth-2-carboxylic acid, in which the phenyl substituents are replaced at the 3 and 4 positions by adamantyl and hydroxyl groups, respectively. It is a selective retinoic acid receptor (RAR) γ agonist that can induce cell cycle arrest and apoptosis in various cancer cells. It functions as both an apoptosis inducer and a retinoic acid receptor γ agonist. CD437 belongs to the adamantane class, monocarboxylic acid class, naphthoic acid class, and phenolic compounds.
CD437 (CAS# 125316-60-1) is a research compound used to study RARγ-mediated signaling and its role in cancer and apoptosis. It is a selective RARγ agonist that induces apoptosis and inhibits tumor growth. It is not approved for clinical use. The compound is also known as AHPN and O-Desmethyl Adapalene. |
| Molecular Formula |
C27H26O3
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|---|---|
| Molecular Weight |
398.49354
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| Exact Mass |
398.188
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| CAS # |
125316-60-1
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| Related CAS # |
CD437-13C6
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| PubChem CID |
135411
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
595.0±50.0 °C at 760 mmHg
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| Melting Point |
271.6-276ºC
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| Flash Point |
327.7±26.6 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.689
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| LogP |
7.45
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LDGIHZJOIQSHPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H26O3/c28-25-6-5-22(20-1-2-21-11-23(26(29)30)4-3-19(21)10-20)12-24(25)27-13-16-7-17(14-27)9-18(8-16)15-27/h1-6,10-12,16-18,28H,7-9,13-15H2,(H,29,30)
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| Chemical Name |
6-[3-(1-adamantyl)-4-hydroxyphenyl]naphthalene-2-carboxylic acid
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| Synonyms |
CD-437 CD 437 CD437
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~150 mg/mL (~376.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 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 25.0 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: 2.5 mg/mL (6.27 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.27 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 | 2.5095 mL | 12.5474 mL | 25.0947 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 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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