PROTAC EML4-ALK Degrader-2

Name: PROTAC EML4-ALK Degrader-2
Brand: TargetMol
SKU: T217191
Rating: 4.5 (1 reviews)

Catalog No. T217191 Copy Product Info

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PROTACEML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. It demonstrates potent selective inhibitory activity against ALK with an IC50 of 1.6 nM. PROTACEML4-ALK also shows selectivity for IGF1R, INSR, FLT3, and FGFR2. Both in vitro and in vivo, PROTACEML4-ALK Degrader-2 exhibits anticancer properties. This compound is applicable in research related to non-small cell lung cancer (NSLC), lung cancer, and cervical cancer.

PROTAC EML4-ALK Degrader-2

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Catalog No. T217191

PROTAC EML4-ALK Degrader-2

Cas No. 2417174-28-6

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	PROTACEML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. It demonstrates potent selective inhibitory activity against ALK with an IC50 of 1.6 nM. PROTACEML4-ALK also shows selectivity for IGF1R, INSR, FLT3, and FGFR2. Both in vitro and in vivo, PROTACEML4-ALK Degrader-2 exhibits anticancer properties. This compound is applicable in research related to non-small cell lung cancer (NSLC), lung cancer, and cervical cancer.
In vitro	PROTAC EML4-ALK Degrader-2 (compound B3) does not increase toxicity to normal cells in the human liver cell line LO2 and demonstrates antiproliferative effects in H3122, H2228, H1299, A549, and HeLa cells, with IC50 values of 0.3, 0.9, 2.84, 1.6, and 1.18 μM, respectively. At concentrations of 0-50 nM over up to 32 hours, it reduces ALK fusion protein levels in H3122 cells in a concentration- and time-dependent manner. This compound shows high selectivity for ALK and moderate inhibitory activity against IGF1R and INSR without inducing their degradation. However, it is not effective against ALK-resistant mutations and shows slightly better activity than LDK378 in BaF3-ALK-L1196M cells.
In vivo	PROTAC EML4-ALK Degrader-2 (compound B3) administered orally at 25-50 mg/kg once daily for 15 days effectively inhibits tumor growth in a dose-dependent manner with good safety in the H3122 xenograft mouse model.

Chemical Properties

Molecular Weight	1060.66
Formula	C₅₂H₆₆ClN₉O₁₁S
Cas No.	2417174-28-6
Smiles	O=C1NC(=O)C(N2C(=O)C=3C=CC=C(NCCOCCOCCOCCNC(=O)CCN4CCC(C5=CC(OC(C)C)=C(C=C5C)NC6=NC=C(Cl)C(=N6)NC=7C=CC=CC7S(=O)(=O)C(C)C)CC4)C3C2=O)CC1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc