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5mg |
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25mg |
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100mg |
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250mg |
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Purity: ≥98%
Belotecan HCl (CKD-602), the hydrochloride of CKD602 which is a Topoisomerase I inhibitor, is a semi-synthetic camptothecin analogue with potential antitumor activity. Belotecan binds to topoisomerase I and inhibits its activity, stabilizing the cleavable complex of topoisomerase I-DNA and preventing topoisomerase I from religating single-stranded DNA breaks. Lethal double-stranded DNA breaks happen when the DNA replication machinery comes into contact with the top technicaloisomerase I-DNA complex, disrupting DNA replication and causing the tumor cell to undergo apoptosis. During DNA replication, reversible single-strand breaks in DNA are mediated by the enzyme topoisomerase I.
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ln Vitro |
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ln Vivo |
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Cell Assay |
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Animal Protocol |
Mice: Belotecan is administered intraperitoneally to groups A and B at doses of 40 mg/kg, 60 mg/kg, and 0 mg/kg (control group) in order to treat established U87MG gliomas in naked mice. After that, for a total of four doses, the dose is repeated once every four days. Histological measurements of the tumor volume reveal the presence of apoptosis[1].
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References |
[4]. Lesser Toxicities of Belotecan in Patients with Small Cell Lung Cancer: A Retrospective Single-Center Study of Camptothecin Analogs. Can Respir J. 2016;2016:3576201. |
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Additional Infomation |
Belotecan Hydrochloride is the hydrochloride salt of the semi-synthetic camptothecin analogue belotecan with potential antitumor activity. Belotecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Topoisomerase I is an enzyme that mediates reversible single-strand breaks in DNA during DNA replication.
See also: Belotecan (annotation moved to). |
Molecular Formula |
C25H28CLN3O4
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Molecular Weight |
469.9605
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Exact Mass |
469.177
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Elemental Analysis |
C, 63.89; H, 6.01; Cl, 7.54; N, 8.94; O, 13.62
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CAS # |
213819-48-8
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Related CAS # |
256411-32-2; 213819-48-8 (HCl)
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PubChem CID |
6918340
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Appearance |
White to yellow solid powder
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Boiling Point |
772.4ºC at 760mmHg
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Flash Point |
420.9ºC
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Vapour Pressure |
4.21E-25mmHg at 25°C
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LogP |
3.813
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Hydrogen Bond Donor Count |
3
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
5
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Heavy Atom Count |
33
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Complexity |
865
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Defined Atom Stereocenter Count |
1
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SMILES |
Cl[H].O1C([C@](C([H])([H])C([H])([H])[H])(C2C([H])=C3C4C(=C(C5=C([H])C([H])=C([H])C([H])=C5N=4)C([H])([H])C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])N3C(C=2C1([H])[H])=O)O[H])=O
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InChi Key |
SJKBXKKZBKCHET-UQIIZPHYSA-N
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InChi Code |
InChI=1S/C25H27N3O4.ClH/c1-4-25(31)19-11-21-22-17(12-28(21)23(29)18(19)13-32-24(25)30)15(9-10-26-14(2)3)16-7-5-6-8-20(16)27-22;/h5-8,11,14,26,31H,4,9-10,12-13H2,1-3H3;1H/t25-;/m0./s1
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Chemical Name |
(19S)-19-ethyl-19-hydroxy-10-[2-(propan-2-ylamino)ethyl]-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione;hydrochloride
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Synonyms |
CKD-602; Camtobell; Belotecan Hydrochloride; 213819-48-8; Camtobell hydrochloride; Belotecan HCl; CKD-602; CKD 602; Belotecan (hydrochloride); (S)-4-ethyl-4-hydroxy-11-(2-(isopropylamino)ethyl)-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione hydrochloride;CKD 602; CKD602; Belotecan
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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: 12.5~47 mg/mL (26.6~100.0 mM)
Water: ~4 mg/mL |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1278 mL | 10.6392 mL | 21.2784 mL | |
5 mM | 0.4256 mL | 2.1278 mL | 4.2557 mL | |
10 mM | 0.2128 mL | 1.0639 mL | 2.1278 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00430144 | Completed | Drug: Belotecan (CKD-602) |
Cervical Cancer | Sokbom Kang | January 2007 | Phase 2 |
NCT01630018 | Completed | Drug: Belotecan Drug: Topotecan |
Epithelial Ovarian Cancer | Chong Kun Dang Pharmaceutical | January 2011 | Phase 2 |
NCT00826644 | Completed | Drug: Belotecan Drug: Etoposide |
Carcinoma, Small Cell | Chonnam National University Hospital |
January 2009 | Phase 3 |
NCT00177281 | Completed | Drug: S CKD602 | Cancer | University of Pittsburgh | September 2003 | Phase 1 |
NCT00754858 | Completed | Drug: belotecan hydrochloride Drug: cisplatin |
Lung Cancer | Yonsei University | May 2010 | Phase 2 |