| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
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| 100mg | |||
| Other Sizes |
| Targets |
Topoisomerase I [1]
|
|---|---|
| ln Vitro |
MCPT inhibited the viability of murine sarcoma S180 cells in a dose-dependent manner with an IC50 value of (0.385 ± 0.08) μM after 24 h treatment, while camptothecin (CPT) showed an IC50 value of (0.904 ± 0.14) μM under the same conditions [1].
MCPT induced apoptosis in murine sarcoma S180 cells as determined by Annexin V-FITC/propidium iodide double staining. After 24 h treatment with 0, 0.19, 0.38, and 0.95 μM MCPT, the apoptosis rates increased from 9.5% to 17.27%, 30.14%, and 66.46%, respectively. The number of early and middle apoptotic cells increased in a dose-dependent manner [1]. Real-time PCR analysis showed that MCPT decreased Bcl-2 mRNA levels and increased Bax mRNA levels in murine sarcoma S180 cells. After treatment with 0, 0.19, 0.38, and 0.95 μM MCPT for 24 h, the relative Bax expression increased from 1 to 1.13, 1.82, and 3.79, respectively, while the Bax/Bcl-2 ratio increased from 1 to 1.61, 2.43, and 4.57, respectively [1]. |
| Cell Assay |
Murine sarcoma S180 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum, 100 μg/mL streptomycin and 100 U/mL penicillin at 37°C in a humidified atmosphere containing 5% CO2 [1].
For the MTT cytotoxicity assay, cells were seeded in 96-well plates at a density of 5 × 10³ cells per well and exposed to serial concentrations of MCPT and CPT for 24 h. Then, 5 μL of MTT solution (5 mg/mL) was added to each well and the plates were incubated for another 4 h at 37°C under 5% CO2. The cells were collected and solubilized with 150 μL DMSO for 15 min. The absorbance at 570 nm was determined using an enzyme-linked immunosorbent assay reader [1]. For flow cytometric apoptosis analysis, murine sarcoma S180 cells were treated with 0, 0.19, 0.38, and 0.95 μM MCPT for 24 h. Cells were collected, washed twice with cold phosphate buffered saline, and 2 × 10⁵ cells were resuspended in 500 μL binding buffer, then stained with 5 μL Annexin V-FITC and 5 μL propidium iodide for 10 min at 25°C in the dark. Cell death was quantified by flow cytometry, and data acquisition and analysis were performed using flow cytometry software [1]. For quantitative real-time PCR, total RNA of murine sarcoma S180 cells treated with different concentrations of MCPT for 24 h was extracted using TRIzol reagent. cDNA was synthesized using a reverse transcription kit. Real-time PCR was performed on a sequence detector system using specific primers for Bcl-2 (forward: 5'-CAT TGG GAA GTT TCA AAT CAG C-3', reverse: 5'-CTT TGC ATT CTT GGA CGA GG-3'), Bax (forward: 5'-TTG CTT CAG GGT TTC ATC CA-3', reverse: 5'-CAG CCT TGA GCA CCA GTT TG-3'), and actin (forward: 5'-GTC CAC CGC AAA TGC TTC TA-3', reverse: 5'-TGC TGT CAC CTT CAC CGT TC-3'). The PCR mixture was pre-heated for 2 min at 50°C and 95°C, then underwent 40 cycles of amplification: 95°C for 15 s, 58°C for 15 s, 72°C for 45 s, and a final extension at 72°C for 10 min. All determinations were performed in triplicate [1]. |
| References |
|
| Additional Infomation |
9-Methoxycamptothecin is a pyranoindoquinoline compound. It has been reported to exist in Hedyotis diffusa, Norhabditis nimodii, and other organisms with relevant data.
MCPT is a C9-substituted lipophilic derivative of camptothecin isolated from Nothapodytes foetida (collected from Hubei Province, China). The compound was identified by NMR spectroscopy and LC-MS, with purity over 95%. The IC50 value of MCPT against murine sarcoma S180 cells was (0.385 ± 0.08) μM, showing better antitumor activity than camptothecin (IC50 = 0.904 ± 0.14 μM). The apoptosis rate induced by MCPT at 0.95 μM was 66.46% after 24 h treatment. MCPT increased the Bax/Bcl-2 ratio in a dose-dependent manner, indicating that the mitochondria pathway may be involved in MCPT-induced apoptosis. The study suggests that MCPT is a topoisomerase I inhibitor but may also involve additional mechanisms beyond topoisomerase I inhibition [1]. |
| Molecular Formula |
C21H18N2O5
|
|---|---|
| Molecular Weight |
378.38
|
| Exact Mass |
378.121
|
| CAS # |
39026-92-1
|
| PubChem CID |
123617
|
| Appearance |
White to yellow solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
773.1±60.0 °C at 760 mmHg
|
| Melting Point |
223-225 ºC
|
| Flash Point |
421.4±32.9 °C
|
| Vapour Pressure |
0.0±2.8 mmHg at 25°C
|
| Index of Refraction |
1.723
|
| LogP |
2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
28
|
| Complexity |
790
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC=C5OC)N=C4C3=C2)O
|
| InChi Key |
XVMZDZFTCKLZTF-NRFANRHFSA-N
|
| InChi Code |
InChI=1S/C21H18N2O5/c1-3-21(26)14-8-16-18-11(7-12-15(22-18)5-4-6-17(12)27-2)9-23(16)19(24)13(14)10-28-20(21)25/h4-8,26H,3,9-10H2,1-2H3/t21-/m0/s1
|
| Chemical Name |
(S)-4-ethyl-4-hydroxy-10-methoxy-1,12-dihydro-14H-pyrano[3',4'
|
| Synonyms |
NSC 176323 NSC-176323NSC176323 9-Methoxycamptothecin
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~264.28 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (2.19 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 sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 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. Solubility in Formulation 2: ≥ 0.83 mg/mL (2.19 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 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6428 mL | 13.2142 mL | 26.4285 mL | |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2857 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 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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