1. PROTAC JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. PROTACs EGFR
  3. MS39

MS39 (compound 6) is a PROTAC targeting EGFR. MS39 is composed of PROTAC target protein ligand N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine (HY-W109039) (red part), E3 ligase ligand (S,R,S)-AHPC (HY-125845) (blue part) and PROTAC Linker Undecanedioic acid (HY-W014125) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-CO-C9-acid (HY-139345). MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells.

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MS39 Chemical Structure

MS39 Chemical Structure

CAS No. : 2675490-92-1

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Description

MS39 (compound 6) is a PROTAC targeting EGFR. MS39 is composed of PROTAC target protein ligand N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine (HY-W109039) (red part), E3 ligase ligand (S,R,S)-AHPC (HY-125845) (blue part) and PROTAC Linker Undecanedioic acid (HY-W014125) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-CO-C9-acid (HY-139345). MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells[1].

Cellular Effect
Cell Line Type Value Description References
HCC827 GI50
0.23 μM
Compound: 2; MS39
Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 3 days by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 3 days by CCK-8 assay
[PMID: 35675209]
Molecular Weight

1056.72

Formula

C55H71ClFN9O7S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC(C(OCCCN1CCN(CC1)C(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)=O)=O)=O)=C5)=CC6=C5C(NC7=CC(Cl)=C(C=C7)F)=NC=N6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (94.63 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 0.9463 mL 4.7316 mL 9.4632 mL
5 mM 0.1893 mL 0.9463 mL 1.8926 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 (protect from light, 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.

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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 (protect from light, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9463 mL 4.7316 mL 9.4632 mL 23.6581 mL
5 mM 0.1893 mL 0.9463 mL 1.8926 mL 4.7316 mL
10 mM 0.0946 mL 0.4732 mL 0.9463 mL 2.3658 mL
15 mM 0.0631 mL 0.3154 mL 0.6309 mL 1.5772 mL
20 mM 0.0473 mL 0.2366 mL 0.4732 mL 1.1829 mL
25 mM 0.0379 mL 0.1893 mL 0.3785 mL 0.9463 mL
30 mM 0.0315 mL 0.1577 mL 0.3154 mL 0.7886 mL
40 mM 0.0237 mL 0.1183 mL 0.2366 mL 0.5915 mL
50 mM 0.0189 mL 0.0946 mL 0.1893 mL 0.4732 mL
60 mM 0.0158 mL 0.0789 mL 0.1577 mL 0.3943 mL
80 mM 0.0118 mL 0.0591 mL 0.1183 mL 0.2957 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.

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Product Name:
MS39
Cat. No.:
HY-157581
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