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CL2A-SN-38 [1279680-68-0]

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Referência HY-128946-1mg

Tamanho : 1mg

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Marca : MedChemExpress

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Contactar o distribuidor local :

Telefone : +1 850 650 7790

Description

CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects^[1].

IC₅₀ & Target

Camptothecins

In Vivo

CL2A-SN-38 coupled to the anti-Trop-2 humanized antibody hRS7 (intraperitoneal injection, 0.2 or 0.4 mg/kg, twice weekly, 4 weeks) can both significantly inhibit tumor growth in mice with human colon (COLO 205) or pancreatic (Capan-1) tumour xenografts^[2].

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

Masse moléculaire

1480.61

Formule

C₇₃H₉₇N₁₁O₂₂

CAS No.

1279680-68-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O[C@](C1=C(CO2)C(N3CC4=C(CC)C5=CC(O)=CC=C5N=C4C3=C1)=O)(CC)C2=O)OCC6=CC=C(NC([C@H](CCCCN)NC(COCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCN7N=NC(CNC(C8CCC(CN9C(C=CC9=O)=O)CC8)=O)=C7)=O)=O)=O)C=C6

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (67.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.6754 mL	3.3770 mL	6.7540 mL
5 mM	0.1351 mL	0.6754 mL	1.3508 mL
10 mM	0.0675 mL	0.3377 mL	0.6754 mL

View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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: 2.08 mg/mL (1.40 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.07%

Fiche technique (274 KB) SDS (479 KB)

COA (252 KB) RP-HPLC (257 KB) LCMS (97 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Cardillo TM, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. [Content Brief]

[2]. Thomas M Cardillo, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. [Content Brief]

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