1. PROTAC Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  2. PROTACs SHP2 Phosphatase
  3. SHP2-D26

SHP2-D26 is a first, potent and effective SHP2 PROTAC degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent. SHP2-D26 can be used for the study of esophageal cancer and acute myeloid leukemia (Pink: SHP2 ligand (HY-176797); Blue: VHL ligand (HY-150803); Black: linker).

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CAS 番号 : 2458219-65-1

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 1288 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1288 在庫あり
Solid
1 mg $286 在庫あり
5 mg $630 在庫あり
10 mg $1050 在庫あり
25 mg $2210 在庫あり
50 mg $3543 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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製品説明

SHP2-D26 is a first, potent and effective SHP2 PROTAC degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent. SHP2-D26 can be used for the study of esophageal cancer and acute myeloid leukemia (Pink: SHP2 ligand (HY-176797); Blue: VHL ligand (HY-150803); Black: linker)[1].

IC50 & Target

SHP2[1]

Cellular Effect
Cell Line Type Value Description References
MV4-11 DC50
2.6 nM
Compound: 26; SHP2-D26
Protac activity at VHL1/SHP2 in human MV4-11 cells assessed as induction of SHP2 degradation measured after 12 hrs by Western blot analysis
Protac activity at VHL1/SHP2 in human MV4-11 cells assessed as induction of SHP2 degradation measured after 12 hrs by Western blot analysis
[PMID: 32437146]
MV4-11 IC50
9.9 nM
Compound: 26; SHP2-D26
Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay
Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay
[PMID: 32437146]
体外実験

SHP2-D26 (0, 3, 10, 30, 100, 300 nM; 12 hours) effectively reduces SHP2 protein in a dosedependent manner, with DC50 values of 6.0 nM, 2.6 nM in KYSE520 and MV-4-11 cells, respectively[1].
SHP2-D26 (100 nM; 0, 2, 4, 8, 12, 24 hours) reduces the SHP2 protein level within 4 h and completes SHP2 depletion with 8 h in KYSE520 and MV-4-11 cells[1].
SHP2-D26 (0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells; 4 days) achieves IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively[1].

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

Cell Proliferation Assay[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells
Incubation Time: 4 days
Result: Achieved IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 12 hours
Result: Reduced SHP2 protein in a dosedependent manner, with DC50 values of 6.0 and 2.6 nM in KYSE520 and MV-4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 100 nM
Incubation Time: 0, 2, 4, 8, 12, 24 hours
Result: Reduced the SHP2 protein level within 4 h and completed SHP2 depletion with 8 h.
分子量

1115.89

分子式

C56H79ClN12O6S2

CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC(C(SC1=NC=C(N2CCC(N)(CC2)C)N=C1N)=CC=C3)=C3NC(CCC(N(CC4)CCN4CCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O)=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 : 83.33 mg/mL (74.68 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 0.8961 mL 4.4807 mL 8.9615 mL
5 mM 0.1792 mL 0.8961 mL 1.7923 mL
10 mM 0.0896 mL 0.4481 mL 0.8961 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.

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純度とドキュメンテーション
参考文献

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8961 mL 4.4807 mL 8.9615 mL 22.4036 mL
5 mM 0.1792 mL 0.8961 mL 1.7923 mL 4.4807 mL
10 mM 0.0896 mL 0.4481 mL 0.8961 mL 2.2404 mL
15 mM 0.0597 mL 0.2987 mL 0.5974 mL 1.4936 mL
20 mM 0.0448 mL 0.2240 mL 0.4481 mL 1.1202 mL
25 mM 0.0358 mL 0.1792 mL 0.3585 mL 0.8961 mL
30 mM 0.0299 mL 0.1494 mL 0.2987 mL 0.7468 mL
40 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5601 mL
50 mM 0.0179 mL 0.0896 mL 0.1792 mL 0.4481 mL
60 mM 0.0149 mL 0.0747 mL 0.1494 mL 0.3734 mL
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The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

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Help & FAQs
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
SHP2-D26
製品番号:
HY-145162
数量:
MCE 日本正規代理店: