Size | Price | Stock | Qty |
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10mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
CZ-48 is a DNA topoisomerase inhibitor potentially for the treatment of solid tumours and lymphoma. CZ-48 is an esterification product from the reaction of natural camptothecin with propionic anhydride.
ln Vivo |
In the CLO-breast cancer (100 mg/kg) and PC3-prostate cancer (1000 mg/kg) anticancer activity) mouse model, camptothecin-20(S)-O-propionate (CZ48, gavage, 100 to 2000 mg/kg/day) has antitumor activity [3].
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Animal Protocol |
Animal/Disease Models: tumor xenografts (size, ∼1 cm3) grown in nude mice [3].
Doses: 100-1000 mg/kg/day. Route of Administration: po (oral gavage) for 2, 4 and 6 days Experimental Results: Anti-tumor effect. |
References |
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Molecular Formula |
C23H20N2O5
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Molecular Weight |
404.422
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Exact Mass |
404.137
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CAS # |
194414-69-2
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Related CAS # |
Camptothecin-20(S)-O-propionate hydrate;1147090-70-7
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PubChem CID |
9887472
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Appearance |
Off-white to gray solid powder
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LogP |
3.04
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
4
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Heavy Atom Count |
30
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Complexity |
862
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Defined Atom Stereocenter Count |
1
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SMILES |
CCC(=O)O[C@]1(C2=C(COC1=O)C(=O)N3CC4=CC5=CC=CC=C5N=C4C3=C2)CC
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InChi Key |
YCNIQYLWIPCLNY-QHCPKHFHSA-N
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InChi Code |
InChI=1S/C23H20N2O5/c1-3-19(26)30-23(4-2)16-10-18-20-14(9-13-7-5-6-8-17(13)24-20)11-25(18)21(27)15(16)12-29-22(23)28/h5-10H,3-4,11-12H2,1-2H3/t23-/m0/s1
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Chemical Name |
(S)-4-ethyl-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4'
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Synonyms |
CZ-48 CZ 48 CZ48
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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 : ~9.09 mg/mL (~22.48 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 | 2.4727 mL | 12.3634 mL | 24.7268 mL | |
5 mM | 0.4945 mL | 2.4727 mL | 4.9454 mL | |
10 mM | 0.2473 mL | 1.2363 mL | 2.4727 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 |
NCT00947739 | Completed | Drug: Camptothecin- 20-O-Propionate Hydrate |
Advanced Solid Tumors Lymphomas |
New Mexico Cancer Care Alliance |
September 2008 | Phase 1 |
NCT02575638 | Unknown | Drug: CZ48 | Solid Tumor | Cao Pharmaceuticals Inc. | July 2008 | Phase 1 |
The three-dimensional structure of CZ48. A, ORTEP diagram of a single molecule of C23H20N2O5·3H2O. One molecule of CZ48 is linked to three molecules of water through strong hydrogen bonds. All of the molecules in a crystal unit are linked to each other through a bridge made of H2O molecules. B, ORTEP diagram of a dimer, [C23H20N2O5·3H2O]2, showing how two molecules of CZ48 are linked by a water bridge. Cancer Res. 2009 Jun 1;69(11):4742-9. td> |
A, correlations between dose levels and the corresponding inhibitions. Three groups of tumor-bearing mice were treated with 100, 200, and 300 mg/kg/d of CZ48, respectively. The mean of the tumor sizes of each group measured at each time point was plotted versus treatment time. B, body weight changes in healthy mice during 280 d of the treatment. The test group was treated with 2,000 mg/kg/d CZ48 (suspended in cottonseed oil) daily for the duration of the treatment period by gavage. The control group was treated by the cottonseed oil only, also daily for the duration of treatment period by gavage. C, antitumor activity of commercial CPT-11 against human SPA lung carcinoma with oral administration of 8 mg/kg/d. This dose was safe to animals treated under our experimental conditions. Under this dose level, CPT-11 did not show significant inhibitory effects. D, antitumor activity of CZ48 against human SPA lung carcinoma with oral administration of 300 mg/kg/d. Under this dose level, CZ48 was effective and showed great inhibitions . Cancer Res. 2009 Jun 1;69(11):4742-9. td> |