SHP2 protein degrader-1

Name: SHP2 protein degrader-1
Brand: MedChemExpress
SKU: HY-145159
Rating: 4.5 (0 reviews)

製品番号: HY-145159 純度: 98.94%: Data Sheet SDS COA 取扱説明書
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SHP2 protein degrader-1 is a potent allosteric inhibitor and a PROTAC degrader of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases.
(Pink: SHP2 ligand (HY-176795); Blue: Cereblon ligand (HY-41547); Black: linker (HY-141015)).

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

SHP2 protein degrader-1 構造式

CAS 番号 : 2624181-69-5

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 2429	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 2429	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$485	在庫あり	Estimated Time of Arrival: December 31
5 mg	$1215	在庫あり	Estimated Time of Arrival: December 31
10 mg		お問い合わせ
50 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 0 publication(s) in Google Scholar

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

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

SHP2 protein degrader-1 is a potent allosteric inhibitor and a PROTAC degrader of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases^[1]. (Pink: SHP2 ligand (HY-176795); Blue: Cereblon ligand (HY-41547); Black: linker (HY-141015)).

IC₅₀ & Target

SHP2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	4.3 μM Compound: 9; SP4	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 38788299]

体外実験

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC₅₀ of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)^[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM^[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells^[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38^[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity^[1].

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

Cell Viability Assay^[1]

Cell Line:	Hela cells
Concentration:	0-200 μM
Incubation Time:	24 hours
Result:	Strongly inhibited the growth of Hela cells, with IC₅₀ of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis^[1]

Cell Line:	Hela cells
Concentration:	0-100 μM
Incubation Time:	96 hours
Result:	Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis^[1]

Cell Line:	Hela cells
Concentration:	0-100 μM
Incubation Time:	96 hours
Result:	Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis^[1]

Cell Line:	Hela cells
Concentration:	0-100 μM
Incubation Time:	96 hours
Result:	Significantly inhibited the phosphorylation of JNK, Erk and p38.

分子量

908.83

分子式

C₄₂H₅₁Cl₂N₁₁O₈

CAS 番号

2624181-69-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCOCCOCCOCCOCCN4N=NC(CNC5(CCN(CC5)C6=CN=C(C7=C(Cl)C(Cl)=CC=C7)C(N)=N6)C)=C4)=CC=C3)=O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 110 mg/mL (121.03 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	1.1003 mL	5.5016 mL	11.0032 mL
5 mM	0.2201 mL	1.1003 mL	2.2006 mL
10 mM	0.1100 mL	0.5502 mL	1.1003 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. 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）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 98.94%

Select Batch:

データシート (271 KB) SDS (251 KB)

COA (244 KB) HNMR (315 KB) RP-HPLC (273 KB) MS (73 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Zheng M, et al. Novel PROTACs for degradation of SHP2 protein. Bioorg Chem. 2021;110:104788. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.1003 mL	5.5016 mL	11.0032 mL	27.5079 mL
	5 mM	0.2201 mL	1.1003 mL	2.2006 mL	5.5016 mL
	10 mM	0.1100 mL	0.5502 mL	1.1003 mL	2.7508 mL
	15 mM	0.0734 mL	0.3668 mL	0.7335 mL	1.8339 mL
	20 mM	0.0550 mL	0.2751 mL	0.5502 mL	1.3754 mL
	25 mM	0.0440 mL	0.2201 mL	0.4401 mL	1.1003 mL
	30 mM	0.0367 mL	0.1834 mL	0.3668 mL	0.9169 mL
	40 mM	0.0275 mL	0.1375 mL	0.2751 mL	0.6877 mL
	50 mM	0.0220 mL	0.1100 mL	0.2201 mL	0.5502 mL
	60 mM	0.0183 mL	0.0917 mL	0.1834 mL	0.4585 mL
	80 mM	0.0138 mL	0.0688 mL	0.1375 mL	0.3438 mL
	100 mM	0.0110 mL	0.0550 mL	0.1100 mL	0.2751 mL