Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

PROTAC EGFR degrader 7 (diTFA)

Imprimer

Référence HY-147858A-25mg

Conditionnement : 25mg

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Téléphone : +1 850 650 7790

Marque : MedChemExpress

Contactez votre distributeur local :

Téléphone : +1 850 650 7790

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC₅₀ of 13.2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC₅₀ of 46.82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research.

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PROTAC EGFR degrader 7 diTFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

Other Forms of PROTAC EGFR degrader 7 diTFA:

PROTAC EGFR degrader 7 In-stock

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Description

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC₅₀ of 13^[1].2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC₅₀ of 46^[1].82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research^[1].

Masse moléculaire

1064.98

Formule

C₅₀H₅₀F₆N₁₀O₁₀

Appearance

Solid

Color

Light yellow to yellow

SMILES

C#CCN(CCN(C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC(C3=CN(C4=CC=CC=C34)C)=CC=N2)C)CCCC(NC5=C6CN(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (93.90 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	0.9390 mL	4.6949 mL	9.3898 mL
5 mM	0.1878 mL	0.9390 mL	1.8780 mL
10 mM	0.0939 mL	0.4695 mL	0.9390 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité
Calculateur de dilution

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.5 mg/mL (2.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (2.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureté et documentation

Purity: 99.19%

Select Batch:

Fiche technique (272 KB) SDS (252 KB)

COA (249 KB) HNMR (248 KB) RP-HPLC (243 KB) LCMS (97 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Zhang W, et al. Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo. Eur J Med Chem. 2022 Aug 5;238:114509. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.9390 mL	4.6949 mL	9.3898 mL	23.4746 mL
	5 mM	0.1878 mL	0.9390 mL	1.8780 mL	4.6949 mL
	10 mM	0.0939 mL	0.4695 mL	0.9390 mL	2.3475 mL
	15 mM	0.0626 mL	0.3130 mL	0.6260 mL	1.5650 mL
	20 mM	0.0469 mL	0.2347 mL	0.4695 mL	1.1737 mL
	25 mM	0.0376 mL	0.1878 mL	0.3756 mL	0.9390 mL
	30 mM	0.0313 mL	0.1565 mL	0.3130 mL	0.7825 mL
	40 mM	0.0235 mL	0.1174 mL	0.2347 mL	0.5869 mL
	50 mM	0.0188 mL	0.0939 mL	0.1878 mL	0.4695 mL
	60 mM	0.0156 mL	0.0782 mL	0.1565 mL	0.3912 mL
	80 mM	0.0117 mL	0.0587 mL	0.1174 mL	0.2934 mL