Art. -Nr.: HY-N6670

Cefotetan

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Cefotetan is a binding agent that targets human Raf1 kinase inhibitor protein (hRKIP). Cefotetan binds to hRKIP, reduces the binding space between hRKIP and Raf1 kinase, relieves hRKIP's inhibition of the Ras/Raf1/MEK/ERK signaling pathway, and enhances ERK phosphorylation. Cefotetan can be used to study diseases associated with dysregulated Ras/Raf1/MEK/ERK signaling pathways. Cefotetan is also a broad-spectrum antibacterial agent that disrupts cell wall synthesis by binding to bacterial penicillin-binding proteins (PBPs). It is used to study bacterial infections such as bone, skin, urinary tract, and lower respiratory tract.

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Reinheit: 98.52%
CAS. Nr.: 69712-56-7
Formel: C₁₇H₁₇N₇O₈S₄
Molecular Weight:575.62

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cefotetan Chemical Structure

CAS. Nr.: 69712-56-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

β-lactam

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Alle Raf Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle Ras Isoform-spezifische Produkte anzeigen :

Alle MEK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	CC₅₀	>32 μg/mL Compound: Cefotetan	Cytotoxicity against HEK293 cells incubated for 20 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells incubated for 20 hrs by resazurin dye based assay	[PMID: 38112278]

In Vitro

Cefotetan (20-80 μM; 30 min) significantly increases HEK293T and HeLa cells ERK phosphorylation levels, and this effect is more pronounced in cells overexpressing hRKIP^[1].
Cefotetan is active against both Gram-positive bacteria (such as Staphylococci and Streptococci) and Gram-negative bacteria (such as Enterobacter and Haemophilus influenzae), and is highly stable against plasmid- and chromosome-mediated β-lactamases. 0.5 mg/L Cefotetan inhibits 75% of Enterobacter, 4 mg/L Cefotetan inhibits 90% of Enterobacter, and the MIC of Cefotetan against Neisseria gonorrhoeae is 0.06-2 mg/L^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

HEK293T cells, HeLa cells, hRKIP-transferred HEK293T cells, hRKIP-transferred HeLa cells
Concentration:

0 μM, 20 μM, 40 μM, 80 μM
Incubation Time:

30 min
Result:

Enhanced the phosphorylation level of ERK dose-dependently.
In hRKIP-transferred HEK293T cells, increased the phosphorylation level of ERK by approximately 300% compared with the control at 80 μM; in hRKIP-transferred HeLa cells, increased the phosphorylation level of ERK by approximately 250% under the same concentration.

In Vivo

Cefotetan (20, 50, 100 mg/kg; i.v.; single dose) shows that plasma drug concentrations increased with dose in animal models such as mice, rats, dogs and monkeys, with the highest concentration in the kidneys. The urinary excretion rate is 50%-74%, and the biliary excretion rate in rats could reach 48%^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice (ICR strain, male, 6-7 weeks old), rats (SD strain, male, 6-9 weeks old), rabbits (white rabbits, male, 3.0-3.5 kg), dogs (female beagle dogs, 9.0-14.0 kg), monkeys (female rhesus monkeys, 4.8-5.6 kg)^[3]
Dosage:

20 mg/kg
Administration:

Intravenous injection, single dose
Result:

Mice: 5 minutes after intravenous injection, the plasma concentration reached 52.3 μg/ml, with the highest renal concentration (58.5 μg/g), 24-hour urinary excretion rate of 67.2%, fecal excretion rate of 30.3%; after subcutaneous injection, the fecal excretion rate was 30.3%, and no active metabolites were detected in urine.
Rats: Plasma concentration increased with increasing dose (20 mg/kg group reached 66.5 μg/ml in 5 minutes), with the highest kidney concentration (100 mg/kg group reached 596 μg/g in 5 minutes), 24-hour urine excretion rate of 51.9%, bile excretion rate of 48.1%, and fecal excretion rate of 37.7%.
Rabbit: Plasma concentration of 83 μg/ml in 5 minutes, 74% in 24-hour urine excretion rate, 5.1% in bile excretion rate, and only 0.3% in feces.
Dog: Plasma concentration of 105 μg/ml in 20 mg/kg group in 5 minutes, with the highest kidney concentration (60.3 μg/g in 30 minutes), 52.8% in 24-hour urine excretion rate, 17.4% in bile excretion rate, and 13.3% in feces.
Monkey: 5-minute plasma concentration 129 μg/ml, 24-hour urine excretion rate 59.7%, bile excretion rate not clearly detected, fecal excretion rate 0.3%, plasma protein binding rate 87%.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 69712-56-7
Appearance Solid
Molecular Weight 575.62
Formel C₁₇H₁₇N₇O₈S₄
Color White to off-white
SMILES

O=C(C(N12)=C(CSC3=NN=NN3C)CS[C@]2([H])[C@](OC)(NC(C(S/4)SC4=C(C(O)=O)/C(N)=O)=O)C1=O)O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 175 mg/mL (304.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7373 mL

8.6863 mL

17.3726 mL

5 mM

0.3475 mL

1.7373 mL

3.4745 mL

10 mM

0.1737 mL

0.8686 mL

1.7373 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (2.17 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (2.17 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.17 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Guo C, et al. Cefotetan-bound human RKIP involves in Ras/Raf1/MEK/ERK signaling pathway. Acta Biochim Biophys Sin (Shanghai). 2022 Dec 25;54(12):1917-1923. [Content Brief]

[2]. Phillips I, et al. Cefotetan: in-vitro antibacterial activity and susceptibility to beta-lactamases. J Antimicrob Chemother. 1983 Jan;11 Suppl:1-9. [Content Brief]

[3]. Komiya M. et al. Absorption, distribution, metabolism, and excretion of cefotetan (YM09330) in experimental animals[J]. Chemotherapy, 1982, 30(Supplement1): 106-118.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7373 mL	8.6863 mL	17.3726 mL	43.4314 mL
	5 mM	0.3475 mL	1.7373 mL	3.4745 mL	8.6863 mL
	10 mM	0.1737 mL	0.8686 mL	1.7373 mL	4.3431 mL
	15 mM	0.1158 mL	0.5791 mL	1.1582 mL	2.8954 mL
	20 mM	0.0869 mL	0.4343 mL	0.8686 mL	2.1716 mL
	25 mM	0.0695 mL	0.3475 mL	0.6949 mL	1.7373 mL
	30 mM	0.0579 mL	0.2895 mL	0.5791 mL	1.4477 mL
	40 mM	0.0434 mL	0.2172 mL	0.4343 mL	1.0858 mL
	50 mM	0.0347 mL	0.1737 mL	0.3475 mL	0.8686 mL
	60 mM	0.0290 mL	0.1448 mL	0.2895 mL	0.7239 mL
	80 mM	0.0217 mL	0.1086 mL	0.2172 mL	0.5429 mL
	100 mM	0.0174 mL	0.0869 mL	0.1737 mL	0.4343 mL

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Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle Raf Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Alle Ras Isoform-spezifische Produkte anzeigen

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cefotetan Related Classifications

HY-N6670 Related Classifications