| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| Targets |
CYP3A4(IC50=16.29 μM);CYP2E1(IC50=25.62 μM);CYP2C9(IC50=24.57 μM)
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| ln Vitro |
In human TNBC cells, cepharanthine (CEP) (2 μM, 48 h) induces apoptosis via the mitochondrial pathway and inhibits cell viability and colony formation[2].
In MDA-MB-231 cells, the combination of cepharanthine (2 μM, 48 h) and epirubicin results in impaired mitochondrial function, mitochondrial fission, and apoptosis[2]. Cepharanthine (5 μM, 24 h) significantly increases the apoptosis that anticancer agents induce in K562 cells and potently increases the sensitivity of anticancer agents Vincristine and Doxorubicin[3]. By preventing the acidification of cytoplasmic organelles, cepharanthine (10-50 μM, 0.5-1 h) shifts the distribution of doxorubicin from cytoplasmic vesicles to nucleoplasm in K562 cells[3]. In vitro, cepharanthine (0-50 μM, 30 min) inhibits the cytochrome P450 enzymes CYP3A4, CYP2E1, and CYP2C9 in human liver[4]. Cepharanthine (0–4 μM, 48 hours) inhibits the growth of P. falciparum in the ring stage, with IC50 values for FCM29, W2, 3D7, and K1 of 3.059, 0.927, 2.276, and 1.803 μM, respectively[5]. |
| ln Vivo |
In MDA-MB-231 cell xenografts, cepharanthine (12 mg/kg, i.p., once daily for 36 days) improves the therapeutic efficacy of epirubicin[2].
By preventing leukocyte activation, cepharanthine (10 mg/kg, i.p., single dose) protects rats from LPS-induced pulmonary vascular injury[6]. |
| Cell Assay |
Cell Line: P. falciparum cultivated in type A+ human erythrocytes
Concentration: 2 μM Incubation Time: 48 h Result: inhibited P. falciparum growth in the ring stage, with IC50 values for FCM29, W2, 3D7, and K1 of 3.059, 0.927, 2.276, and 1.803 μM, respectively. |
| Animal Protocol |
MDA-MB-231 cell xenografts in mice[1]
Dosage: 12 mg/kg Administration: Intraperitoneal injection (i.p.), once daily for 36 days Result: When combined with Epirubicin (HY-13624), the therapeutic efficacy was significantly higher than when either drug was administered by itself. |
| References |
| Molecular Formula |
C37H38N2O6
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|---|---|
| Molecular Weight |
606.7074
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| Exact Mass |
606.27
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| Elemental Analysis |
C, 73.25; H, 6.31; N, 4.62; O, 15.82
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| CAS # |
481-49-2
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| Appearance |
white solid powder
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| SMILES |
COC1=CC2=C3C=C1OC4=C(OCO5)C5=CC6=C4[C@@](CC7=CC=C(OC(C(OC)=C8)=CC=C8C[C@@]3([H])N(C)CC2)C=C7)([H])N(C)CC6
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| InChi Key |
RCBDVSWQYYTNLG-WDYNHAJCSA-N
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| InChi Code |
InChI=1S/C37H38N2O6/c1-38-13-11-24-18-32(41-4)33-20-27(24)28(38)16-23-7-10-30(31(17-23)40-3)44-26-8-5-22(6-9-26)15-29-35-25(12-14-39(29)2)19-34-36(37(35)45-33)43-21-42-34/h5-10,17-20,28-29H,11-16,21H2,1-4H3/t28-,29+/m1/s1
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| Chemical Name |
(15S,31R)-36,53-dimethoxy-16,32-dimethyl-15,16,17,18,31,32,33,34-octahydro-2,6-dioxa-1(4,5)-[1,3]dioxolo[4,5-g]isoquinolina-3(7,1)-isoquinolina-5,7(1,4)-dibenzenacyclooctaphane
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| Synonyms |
Cepharanthine; 6',12'-Dimethoxy-2,2'-dimethyl-6,7-[methylenebis- (oxy)]oxyacanthan; Cepharanthin; O-Methylcepharanoline.
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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 |
| 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 : 50~100 mg/mL (82.41~164.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.02 mg/mL (9.92 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (4.12 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: ≥ 2.08 mg/mL (3.43 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. Solubility in Formulation 4: ≥ 2.08 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil 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. Solubility in Formulation 5: 2% DMSO+ 30% PEG300+ 5% Tween 80+ 63% ddH2O: 2mg/ml (3.30mM) Solubility in Formulation 6: 6.02 mg/mL (9.92 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6482 mL | 8.2412 mL | 16.4823 mL | |
| 5 mM | 0.3296 mL | 1.6482 mL | 3.2965 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6482 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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