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| ln Vitro |
Topoisomerase I inhibitor Karenitecin has strong anticancer properties. After two hours of treatment, kénitecin reduced the proliferation of A253 cells with IC10, IC50, and IC90 values of 0.01, 0.07, and 0.7 μM, respectively. In A253 cells, kenditecin causes DNA damage (0.01, 0.07, and 0.7 μM) and raises the expression of the cyclin E and cdk2 proteins (0.07 and 0.7 μM). At low doses, kenditecin dramatically increases the cyclin B/cdc2-related kinase activity, whereas at high concentrations, it modestly suppresses this kinase activity [1]. Several human colon cancer cell lines, including COLO205, COLO320, LS174T, SW1398, and WiDr cells, are inhibited by karyanitecin, with IC50 values of 2.4 nM, 1.5 nM, 1.6 nM, 2.9 nM, and 3.2 nM, respectively [2].
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| ln Vivo |
Karenitecin inhibited the maximal development of COLO320 and COLO205 colon cancer cells by intraperitoneal injection at a dose of 1 mg/kg in mice, 61% and 54%, respectively. Karenitecin (1.0 mg/kg × 5 ip daily) notably reduced the growth inhibition of Pgp-positive and Pgp-negative parental xenografts [2].
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| References |
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| Additional Infomation |
Cositecan is a pyranoindolizinoquinoline.
Cositecan is the novel camptothecin derivative which is also known as Karenitecin. It has been developed for superior oral bioavailability and increased lactone stability. It is used to treat cancer. Cositecan is a synthetic silicon-containing agent related to camptothecin with antineoplastic properties. Cositecan stabilizes the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks and consequently triggering apoptosis. Because it is lipophilic, cositecan exhibits enhanced tissue penetration and bio-availability compared to water-soluble camptothecins. Drug Indication Investigated for use/treatment in brain cancer, lung cancer, and melanoma. Mechanism of Action BNP1350, 7-[(2-trimethylsilyl)ethyl]-20(S)-camptothecin, is a novel semi-synthetic, highly lipophilic, silicon-containing camptothecin and an inhibitor of topoisomerase I. It has been supercomputer engineered for superior oral bioavailability, superior lactone stability, broad anti-tumor activity, increased potency and insensitivity to Pgp/MRP/LRP drug resistance. |
| Molecular Formula |
C25H28N2O4SI
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|---|---|
| Molecular Weight |
448.59
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| Exact Mass |
448.181
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| CAS # |
203923-89-1
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| PubChem CID |
148202
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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 |
727.2±60.0 °C at 760 mmHg
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| Flash Point |
393.6±32.9 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.645
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| LogP |
4.14
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
891
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC=CC=C5N=C4C3=C2)CC[Si](C)(C)C)O
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| InChi Key |
POADTFBBIXOWFJ-VWLOTQADSA-N
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| InChi Code |
InChI=1S/C25H28N2O4Si/c1-5-25(30)19-12-21-22-17(13-27(21)23(28)18(19)14-31-24(25)29)15(10-11-32(2,3)4)16-8-6-7-9-20(16)26-22/h6-9,12,30H,5,10-11,13-14H2,1-4H3/t25-/m0/s1
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| Chemical Name |
(19S)-19-ethyl-19-hydroxy-10-(2-trimethylsilylethyl)-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
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| Synonyms |
Cositecan, 7-Trimethylsilylethylcamptothecin; BNP 1350, BNP1350, BNP-1350, Karenitecin; MCC 12824, MCC-12824, MCC12824, DB 172, DB172, DB-172
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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 : ~3.03 mg/mL (~6.75 mM)
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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 | 2.2292 mL | 11.1460 mL | 22.2921 mL | |
| 5 mM | 0.4458 mL | 2.2292 mL | 4.4584 mL | |
| 10 mM | 0.2229 mL | 1.1146 mL | 2.2292 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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