|Description:||1. (S)-10-Hydroxycamptothecin (OPT), an analog of camptothecin (CPT), was found to inhibit the growth of the mouse hepatoma BW7756, when given at 1.0 mg/kg/day for 14 days; in spite of the narrow range of the effective dose of this drug against mouse hepatoma BW7756, the use of OPT in combination with other antitumor agents may be useful in primary hepatoma or liver metastases in view of its low toxicity towards host liver. |
2. (S)-10-Hydroxycamptothecin, as an inhibitor of the growth of P388 leukemia in mice, is as potent as the parent compound camptothecin (CPT).
|Targets:||TNF-α | P450 (e.g. CYP17) | Topoisomerase|
|Source:||The barks of Camptotheca acuminata Decne|
|Solvent:||Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.|
|Storage:||Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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|After receiving:||The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.|
|1 mg||5 mg||10 mg||20 mg||25 mg|
|1 mM||2.7446 mL||13.7231 mL||27.4461 mL||54.8923 mL||68.6153 mL|
|5 mM||0.5489 mL||2.7446 mL||5.4892 mL||10.9785 mL||13.7231 mL|
|10 mM||0.2745 mL||1.3723 mL||2.7446 mL||5.4892 mL||6.8615 mL|
|50 mM||0.0549 mL||0.2745 mL||0.5489 mL||1.0978 mL||1.3723 mL|
|100 mM||0.0274 mL||0.1372 mL||0.2745 mL||0.5489 mL||0.6862 mL|
Cancer Treat Rep. 1983 Feb;67(2):179-82.
|Action of (S)-10-hydroxycamptothecin on P388 leukemia and distribution of the drug in mice.[Pubmed: 6825126]|
|As an inhibitor of the growth of P388 leukemia in mice, (S)-10-Hydroxycamptothecin (OPT) was as potent as the parent compound camptothecin (CPT). Incorporation of thymidine into DNA was the parameter most sensitive to OPT in vitro (ED50 approximately 4 micrograms/ml), but incorporation of cytidine into RNA and of acetate into lipids was also reduced significantly in the presence of the drug. The cytofluorometric profile suggested suppression of the S and G2/M phases. The distribution of OPT in mice at 2 and 24 hours after ip injection (10 mg/kg) was essentially similar to that of CPT, with the exception of a somewhat greater concentration of CPT in the liver. In their pharmacology, OPT and CPT appear to be very similar, despite reports that the hydroxy derivative is less toxic.|
Int J Pharm. 2014 Apr 25;465(1-2):378-87.
|A novel multifunctional poly(amidoamine) dendrimeric delivery system with superior encapsulation capacity for targeted delivery of the chemotherapy drug 10-hydroxycamptothecin.[Pubmed: 24530519]|
|With the aim of developing an efficient targeted delivery system for cancer therapy that overcomes drug leakage during circulation, we prepared a novel multifunctional dendrimeric carrier by integrating long hydrophobic C₁₂ alkyl chains, poly(ethylene glycol) chains and c(RGDfK) ligands presented on the surface. This dendrimer was able to tightly encapsulate the hydrophobic anticancer drug 10-Hydroxycamptothecin (10-HCPT) through simple complexation and selectively target the drug to cancer cells overexpressing integrin αvβ₃ through high affinity interactions. The complex has a high loading efficiency, with each molecule encapsulating approximately 20 drug molecules; high stability, without any detectable drug release during dialysis for three days; and high water solubility, achieving an approximately 600-fold increase over the water solubility of free 10-Hydroxycamptothecin. This complex exhibited notably high cytotoxicity against 22RV1 cells overexpressing integrin αvβ₃ and a far lower cytotoxicity against MCF-7 cells, which express low levels of integrin αvβ₃. We expected encapsulated 10-Hydroxycamptothecin to regain its anti-cancer activity following selective internalization of the complex into carcinoma cells via integrin receptor mediated endocytosis. As the drug remains inactive before internalization, this carrier has the ability to overcome problems associated with drug leakage in the circulation and off-target effects on normal tissues.|
Bioorg Med Chem. 2015 Jan 1;23(1):118-25.
|Synthesis of novel 10-hydroxycamptothecin derivatives utilizing topotecan hydrochloride as ortho-quinonemethide precursor. [Pubmed: 25481395]|
|A series of 9-(alkylthiomethyl)-10-Hydroxycamptothecins and pyrano-fused camptothecin derivatives were synthesized via the reaction of topotecan hydrochloride with various thiols and alkyl vinyl ethers respectively. In the reactions, topotecan hydrochloride was utilized as ortho-quinonemethide (o-QM) precursor. The configuration of 19 was determined by (1)H NMR and NOESY spectra as syn-isomers, suggesting that the cycloaddition of topotecan with alkyl vinyl ethers could undergo a hetero Diels-Alder reaction. All the synthesized compounds were screened on cancer cell lines HepG2, KB, HCT-8 and SGC7901. Some compounds were selected to assess their inhibitory activity against Topo I via Topo I mediated DNA cleavage assays. The results showed that among those tested 9-(alkylthiomethyl)-10-Hydroxycamptothecins, the compounds with bulkier hydrophobic side chains at 9-position have better bioactivities. As well as all pyrano-fused camptothecins possess antiproliferative activity against the tested cancer cell lines. Docking studies suggested that there are more interactions between the novel analogues and the binding site of Topo I.|
Anticancer Res. 1981;1(2):115-9.
|Anti-tumor effect of (S)-10-hydroxycamptothecin on mouse hepatoma BW7756 and its possible mode of action.[Pubmed: 7347154]|
|(S)-10-Hydroxycamptothecin (OPT), an analog of camptothecin (CPT), was found to inhibit the growth of the mouse hepatoma BW7756, when given at 1.0 mg/kg/day for 14 days. Cell cycle studies using flow cytofluorometry indicated that this drug inhibited the S-Phase of the tumor cells in vivo and the S and G2/M phases in vitro. Similar studies on host liver showed little or no effect. In spite of the narrow range of the effective dose of this drug against mouse hepatoma BW7756, the use of OPT in combination with other antitumor agents may be useful in primary hepatoma or liver metastases in view of its low toxicity towards host liver. A simple cytofluorometric method useful for live cell cycle study has been adapted for this investigation and can be adopted for other drug studies.|