| Size | Price | |
|---|---|---|
| 50mg | ||
| Other Sizes |
| ln Vitro |
In vitro release of pure Sancycline HCl from suspension: in PBS (pH 7.4 and pH 5.6, both with 0.5% Tween 80), approximately 95% of the drug was released within 10 hours, showing a burst release profile. [1]
Cytotoxicity of pure Sancycline HCl against HeLa cells: at 20 µM for 24 h, cell viability was 70.9 ± 7.5%; at 20 µM for 48 h, cell viability was 61.1 ± 4.4%. [1] Morphological changes: HeLa cells treated with 20 µM Sancycline HCl for 6 h showed no obvious effect on cell morphology. [1] |
|---|---|
| Cell Assay |
MTT assay for cytotoxicity: HeLa cells were plated in 96-well plates at 8×10³ cells per well. After 12 h, cells were exposed to various concentrations of Sancycline HCl (including 20 µM) for 24 or 48 h. MTT solution was added to a final concentration of 0.5 mg/mL and incubated for 4 h at 37°C. Formazan crystals were solubilized with 150 µL DMSO, and absorbance was measured at 570 nm with background correction at 630 nm. Untreated cells were taken as 100% viable. [1]
In vitro release assay: Freshly prepared Sancycline HCl suspension (5 mL; 100 µg/mL) was placed into a pre-swelled dialysis bag (7 kDa MW cutoff). The bag was incubated in release medium (PBS pH 7.4 or pH 5.5, 20 mL with 0.5% Tween 80) at 37°C under horizontal shaking. At predetermined time points, the bag was transferred to fresh medium. Released CMT-3 content was determined by HPLC (mobile phase MeOH:H₂O with 0.5% TFA = 30:70, flow rate 1 mL/min, wavelength 360 nm). [1] Cell morphology observation: HeLa cells were seeded in 6-well plates at 3×10⁶ per well. After 12 h, cells were exposed to 20 µM Sancycline HCl for 6 h, and cell morphology was captured by digital camera. [1] |
| References |
Int J Pharm.2013 Jun 25;450(1-2):225-34.
|
| Additional Infomation |
Sancycline HCl (CMT-3) is a 4-demethylaminosancycline derivative of tetracycline. It lacks antimicrobial activity but inhibits matrix metalloproteinases (MMPs). It has shown anti-tumor and anti-metastatic effects in various cancer models (e.g., breast, colon, prostate, melanoma). However, its poor water solubility limits clinical use as a parenteral drug. Adverse effects observed in clinical trials (referenced from other studies) include nausea, vomiting, liver function abnormalities, diarrhea, mucositis, leukopenia, and thrombocytopenia. [1]
|
| Molecular Formula |
C21H23CLN2O7
|
|---|---|
| Molecular Weight |
450.872
|
| Exact Mass |
450.119
|
| CAS # |
6625-20-3
|
| Related CAS # |
6625-20-3 (HCl);808-26-4;
|
| PubChem CID |
54712662
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.61g/cm3
|
| Boiling Point |
639.9ºC at 760 mmHg
|
| Melting Point |
224-228° C (dec.)
|
| Flash Point |
340.8ºC
|
| Index of Refraction |
1.734
|
| LogP |
1.622
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
31
|
| Complexity |
892
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
Cl.OC1=CC=CC2=C1C(=C1[C@@H](C2)C[C@H]2[C@@H](C(C(=C(O)[C@@]2(O)C1=O)C(=O)N)=O)N(C)C)O
|
| InChi Key |
CIJFGLCHAOVWRZ-QKYUADJBSA-N
|
| InChi Code |
InChI=1S/C21H22N2O7.ClH/c1-23(2)15-10-7-9-6-8-4-3-5-11(24)12(8)16(25)13(9)18(27)21(10,30)19(28)14(17(15)26)20(22)29;/h3-5,9-10,15,24-25,28,30H,6-7H2,1-2H3,(H2,22,29);1H/t9-,10-,15-,21-;/m0./s1
|
| Chemical Name |
(4S,4aS,5aR,12aR)-4-(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide;hydrochloride
|
| Synonyms |
GS-2147 NSC-51812 GS21476-Demethyl-6-deoxytetracycline GS 2147 Sancycline HClBonomycin NSC 51812 Sanciclina
|
| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.2179 mL | 11.0897 mL | 22.1793 mL | |
| 5 mM | 0.4436 mL | 2.2179 mL | 4.4359 mL | |
| 10 mM | 0.2218 mL | 1.1090 mL | 2.2179 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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