2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs c-Met/HGFR Apoptosis
  4. PRO-6E

PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)).

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PRO-6E Chemical Structure

PRO-6E Chemical Structure

CAS No. : 2353493-69-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1118 In-stock
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10 mM * 1 mL in DMSO USD 1118 In-stock
Solid
1 mg USD 290 In-stock
5 mg USD 666 In-stock
10 mg USD 1198 In-stock
25 mg USD 2397 In-stock
50 mg USD 4075 In-stock
100 mg USD 6923 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878))[1].

In Vitro

PRO-6E (0.03-10 μM; 48 h) inhibits the cell growth in MKN-45, SNU-638 cells[1].
PRO‐6 E (1 μM; over 24 h) facilitates MET degradation in MKN-45 cells[1].
PRO‐6 E (0.1-1 μM; 48 h) increase in the percentage of G2/M phase cells and decrease in the percentage of S phase cells in MKN-45 cells[1].

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

PRO-6E Related Antibodies

Cell Viability Assay[1]

Cell Line: MKN-45, SNU-638 cells
Concentration: 0, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 48 h
Result: Inhibited the cell growth.

Cell Cycle Analysis[1]

Cell Line: MKN-45 cells
Concentration: 0, 0.1, 0.3, 1, 3 μM
Incubation Time: 48 h
Result: Increased in the percentage of G2/M phase cells and decreased in the percentage of S phase cells.

Western Blot Analysis[1]

Cell Line: MKN-45 cells
Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 12, 24, 36, 48, and 72 h
Result: facilitated MET degradation over 24 hours.
In Vivo

PRO-6E (oral gavage; 30 mg/kg/day for 15 days) inhibits tumor growth in MKN‐45 cell‐derived xenograft tumor model[1].

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

Animal Model: MKN‐45 cell‐derived xenograft tumor model[1]
Dosage: 30 mg/kg/day for 15 days
Administration: Oral gavage
Result: Inhibited tumor growth.
Molecular Weight

848.75

Formula

C42H44Cl2FN7O7
CAS No.
Appearance

Solid

SMILES

O=C1C2=C(OCCCCCCCC(N3CCC(N4C=C(C5=CN=C(N)C(O[C@@H](C6=C(C(F)=CC=C6Cl)Cl)C)=C5)C=N4)CC3)=O)C=CC=C2C(N1C7C(NC(CC7)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (117.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1782 mL 5.8910 mL 11.7820 mL
5 mM 0.2356 mL 1.1782 mL 2.3564 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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In Vivo Dissolution Calculator
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Purity & Documentation
References

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 1.1782 mL 5.8910 mL 11.7820 mL 29.4551 mL
5 mM 0.2356 mL 1.1782 mL 2.3564 mL 5.8910 mL
10 mM 0.1178 mL 0.5891 mL 1.1782 mL 2.9455 mL
15 mM 0.0785 mL 0.3927 mL 0.7855 mL 1.9637 mL
20 mM 0.0589 mL 0.2946 mL 0.5891 mL 1.4728 mL
25 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1782 mL
30 mM 0.0393 mL 0.1964 mL 0.3927 mL 0.9818 mL
40 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7364 mL
50 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5891 mL
60 mM 0.0196 mL 0.0982 mL 0.1964 mL 0.4909 mL
80 mM 0.0147 mL 0.0736 mL 0.1473 mL 0.3682 mL
100 mM 0.0118 mL 0.0589 mL 0.1178 mL 0.2946 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

PRO-6E2353493-69-1PROTACsc-Met/HGFRApoptosisgastric cancerMKN-45SNU‐638cell apoptosisMKN‐45 cell‐derived xenograft tumor modelInhibitorinhibitorinhibit

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