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MYC degrader 1

Name: MYC degrader 1
Brand: TargetMol
SKU: T85534
Price: 148 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T85534 Copy Product Info

Purity: 98.68%

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MYC degrader 1 is an orally bioavailable MYC protein degrader with antitumor activity. It can restore the function of pRB1 protein and re-sensitize MYC-overexpressing tumor cells to CDK4/6 inhibitors.

Cas No. 2946670-96-6

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Pack Size	Price	USA Stock	Global Stock
1 mg	$148	-	In Stock
5 mg	$378	-	In Stock
10 mg	$619	-	In Stock
25 mg	$1,230	-	In Stock
1 mL x 10 mM (in DMSO)	$523	-	In Stock

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

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

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Purity:98.68%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	MYC degrader 1 is an orally bioavailable MYC protein degrader with antitumor activity. It can restore the function of pRB1 protein and re-sensitize MYC-overexpressing tumor cells to CDK4/6 inhibitors.
In vitro	Methods: A variety of tumor cell lines were treated with MYC degrader 1 alone or in combination with Palbociclib. The degradation level of MYC protein, cell proliferation IC₅₀, cell cycle-related genes and colony formation ability were detected. Results: : 1.MYC degrader 1 (0–1000 nM, 24 h) could degrade MYC protein in T24, C4-2, MDA-MB-231, 22RV1, T47D and UMUC14 cells. 2.MYC degrader 1 (10 nM, 24 h) pretreatment could significantly increase the sensitivity of T24 and UMUC14 cells to Palbociclib, and the IC₅₀ of the two decreased from 8.37 μM and 97.39 μM to 3.11 μM and 10.23 μM respectively. 3.MYC degrader 1 (10 nM, 24 h) could synergistically enhance the inhibitory effect of Palbociclib on cell cycle-related genes in drug-resistant tumor cell lines T24, C4-2 and MDA-MB-231, and reduce the ability of cell colony formation [1].
In vivo	Methods: Tumor-bearing mice were orally administrated with MYC degrader 1 alone or in combination with Palbociclib by gavage, and its effects on the growth of T24, UMUC14 and MYC-deficient xenograft tumors were observed. Results: : 1.MYC degrader 1 (6 mg/kg, oral administration, once a day for 7 consecutive days) could significantly inhibit the growth of T24 and UMUC14 xenograft tumors in mice, while exerting no obvious effect on MYC-deficient xenograft tumors. 2.MYC degrader 1 (6 mg/kg, gavage, once a day for 30 consecutive days) could markedly enhance the inhibitory effect of Palbociclib on tumor growth in T24 xenograft mice [1].

Chemical Properties

Molecular Weight	626.07
Formula	C₃₂H₃₁ClF₃N₅O₃
Cas No.	2946670-96-6
Smiles	O=C1NC(=O)C(N2C(=O)C3=CC=C(C=C3C2)CNCC4CCN(C=5N=CC(=CC5C(F)(F)F)C6=CC=CC(Cl)=C6)CC4)CC1

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 80 mg/mL (127.78 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5973 mL	7.9863 mL	15.9727 mL	79.8633 mL
5 mM	0.3195 mL	1.5973 mL	3.1945 mL	15.9727 mL
10 mM	0.1597 mL	0.7986 mL	1.5973 mL	7.9863 mL
20 mM	0.0799 mL	0.3993 mL	0.7986 mL	3.9932 mL
50 mM	0.0319 mL	0.1597 mL	0.3195 mL	1.5973 mL
100 mM	0.0160 mL	0.0799 mL	0.1597 mL	0.7986 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Related Tags: MYC degrader 1 chemical structure | MYC degrader 1 in vivo | MYC degrader 1 in vitro | MYC degrader 1 formula | MYC degrader 1 molecular weight