PROTAC Mcl1 degrader-1

Name: PROTAC Mcl1 degrader-1
Brand: MedChemExpress
SKU: HY-125877
Rating: 4.5 (1 reviews)

製品番号: HY-125877 純度: 98.13%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM.

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PROTAC Mcl1 degrader-1 構造式

CAS 番号 : 2163793-38-0

容量	価格（税別）	在庫状況	数量
5 mg	$233	在庫あり	Estimated Time of Arrival: December 31
10 mg	$388	在庫あり	Estimated Time of Arrival: December 31
25 mg	$815	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1305	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2090	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

顧客検証

•Structure. 2024 Dec 5;32(12):2352-2363.e8. [Abstract]

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Bcl-2 Family アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

Mcl-1

0.78 μM (IC₅₀)

Bcl-2

0.54 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	DC₅₀	0.7 μM Compound: C3	Induction of CRBN-mediated Mcl-1 degradation in human HeLa cells assessed as Mcl-1 removal activity measured at 12 hrs by Western blot analysis Induction of CRBN-mediated Mcl-1 degradation in human HeLa cells assessed as Mcl-1 removal activity measured at 12 hrs by Western blot analysis	[PMID: 31389699]

体外実験

PROTAC Mcl1 degrader-1 (compound C3) induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand Pomalidomide (HY-10984) to Mcl-1 inhibitor S1-6 with μM-range affinity^[1].
PROTAC Mcl1 degrader-1 (0-10 μM; 0-24 h) induces selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells in a time- and concentration-dependent manner^[1].
PROTAC Mcl1 degrader-1 (0-2 μM; 24 h) shows cytotoxicity against H23 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	HeLa cells and H23 cells
Concentration:	0.3, 1.0, 3.0 and 10 μM
Incubation Time:	0-24 h
Result:	Induced time- and concentration-dependent selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells. Induced Mcl-1 depletion and PARP cleavage in H23 cells (0-10 μM; 12 h).

分子量

909.84

分子式

C₄₅H₄₅BrN₆O₈S

CAS 番号

2163793-38-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CC(NCCCCCCNC(CCCCC(NCCN2C(C3=C4C(C2=O)=CC=C(C4=CC=C3)SC5=CC=C(C=C5)Br)=O)=O)=O)=C1C6=O)N6C7CCC(NC7=O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, stored under nitrogen

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

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (54.95 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	1.0991 mL	5.4955 mL	10.9909 mL
5 mM	0.2198 mL	1.0991 mL	2.1982 mL
10 mM	0.1099 mL	0.5495 mL	1.0991 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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 (2.75 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (stored under nitrogen)

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.

純度とドキュメンテーション

純度: 98.13%

Select Batch:

データシート (273 KB) SDS (393 KB)

COA (249 KB) HNMR (273 KB) LCMS (122 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Wang Z, et al. Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands. J Med Chem. 2019 Aug 21. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.0991 mL	5.4955 mL	10.9909 mL	27.4774 mL
	5 mM	0.2198 mL	1.0991 mL	2.1982 mL	5.4955 mL
	10 mM	0.1099 mL	0.5495 mL	1.0991 mL	2.7477 mL
	15 mM	0.0733 mL	0.3664 mL	0.7327 mL	1.8318 mL
	20 mM	0.0550 mL	0.2748 mL	0.5495 mL	1.3739 mL
	25 mM	0.0440 mL	0.2198 mL	0.4396 mL	1.0991 mL
	30 mM	0.0366 mL	0.1832 mL	0.3664 mL	0.9159 mL
	40 mM	0.0275 mL	0.1374 mL	0.2748 mL	0.6869 mL
	50 mM	0.0220 mL	0.1099 mL	0.2198 mL	0.5495 mL