| Size | Price | Stock | Qty |
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| 5mg |
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Cefatrizine (BL-S-640) is a novel and potent elongation factor-2 kinase (eEF2K) inhibitor with anticancer and antibacterial activity. It is also an orally bioactive and broad-spectrum cephalosporin antibiotic.
| ln Vitro |
Cefatrizine (0-100 µM; 24 h) has a dose-dependent, remarkable anti-proliferative effect on MCF-7 and MDA-MB-436 cell growth[1]. Cefatrizine (30 µM; 12 h) causes breast cancer cells to experience ER stress[1]. Cefatrizine (12, 24, and 36 hours) raises the amount of CHOP, a hallmark of ER stress-induced apoptosis, and in MCF-7 and MDA-MB-436 cells, it enhances the expression of key proteins in eEF2K-modulated ER stress pathways, including Bip, p-PERK, XBP-1S, and p-JNK[1].
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| ln Vivo |
In an intracystically infected P. mirabilis model, cefatrizine (BL-S-640) (0.2, 1, 5, 25 mg/kg; po; 4 times daily for 3 days) decreases the number of infecting organisms in the kidneys and bladder[2].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF-7, MDA-MB-436 cells Tested Concentrations: 0-100 µM Incubation Duration: 24 h Experimental Results: Led to a remarkable anti-proliferative effect on cells and resulted in almost 50% inhibition in the MCF-7 and MDA-MB-436 cells when at 33 µM and 29 µM. Cell Viability Assay[1] Cell Types: MCF-7, MDA-MB-436 cells Tested Concentrations: 30 µM Incubation Duration: 12 h Experimental Results: Led to massive cytoplasmic vacuolization. |
| Animal Protocol |
Animal/Disease Models: MaleSwiss-Webster mice (19-21 g; P. mirabilis intracystically infected model)[2].
Doses: 0.2, 1, 5, 25 mg/kg Route of Administration: Oral administration; 4 times daily for 3 days. Experimental Results: decreased the number of infecting organisms to less than 1,000 in the bladder when 1 mg/kg, and in the kidneys when 0.2 mg/kg. |
| References |
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| Additional Infomation |
Cefatrizine is a cephalosporin compound having (1H-1,2,3-triazol-4-ylsulfanyl)methyl and [(2R)-2-amino-2-(4-hydroxyphenyl)]acetamido side-groups. An antibacterial drug first prepared in the 1970s, it has more recently been found to be an inhibitor of eukaryotic elongation factor-2 kinase (eEF2K), which is known to regulate apoptosis, autophagy and ER stress in many types of human cancers. It has a role as an antibacterial drug and an EC 2.7.11.20 (elongation factor 2 kinase) inhibitor. It is a cephalosporin, a semisynthetic derivative, a carboxylic acid, a member of triazoles, a member of phenols and an amino acid amide.
Cefatrizine is a broad-spectrum, semisynthetic, first-generation cephalosporin with antibacterial activity. Cefatrizine binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Orally active semisynthetic cephalosporin antibiotic with broad-spectrum activity. |
| Molecular Formula |
C18H18N6O5S2
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|---|---|
| Molecular Weight |
462.499
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| Exact Mass |
462.078
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| CAS # |
51627-14-6
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| PubChem CID |
6410758
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
948.1±65.0 °C at 760 mmHg
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| Flash Point |
527.2±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.794
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| LogP |
-0.41
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
775
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| Defined Atom Stereocenter Count |
3
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| SMILES |
OC1=CC=C([C@@H](N)C(N[C@@H]2C(N3C(C(O)=O)=C(CS[C@H]23)CSC4=CN=NN4)=O)=O)C=C1
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| InChi Key |
UOCJDOLVGGIYIQ-PBFPGSCMSA-N
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| InChi Code |
InChI=1S/C18H18N6O5S2/c19-12(8-1-3-10(25)4-2-8)15(26)21-13-16(27)24-14(18(28)29)9(7-31-17(13)24)6-30-11-5-20-23-22-11/h1-5,12-13,17,25H,6-7,19H2,(H,21,26)(H,28,29)(H,20,22,23)/t12-,13-,17-/m1/s1
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| Chemical Name |
(6R,7R)-7-[[(2R)-2-amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-(2H-triazol-4-ylsulfanylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
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| Synonyms |
BL S 640 BL-S-640 Cefatrizine
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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) |
H2O : ~250 mg/mL (~540.54 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 | 2.1622 mL | 10.8108 mL | 21.6216 mL | |
| 5 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL | |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1622 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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