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

MS39 (compound 6) is a PROTAC targeting EGFR. MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells.
(Pink: EGFR ligand (HY-W109039); Blue: Ligands for E3 Ligase ligand (HY-125845); Black: linker (HY-W014125)).

For research use only. We do not sell to patients.

MS39

MS39 Chemical Structure

CAS No. : 2675490-92-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

MS39 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

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Description

MS39 (compound 6) is a PROTAC targeting EGFR. MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells[1]. (Pink: EGFR ligand (HY-W109039); Blue: Ligands for E3 Ligase ligand (HY-125845); Black: linker (HY-W014125)).

Cellular Effect
Cell Line Type Value Description References
HCC827 DC50
5 nM
Compound: 6; MS39
Protac activity at VHL/EGFR exon 19 deletion mutant in human HCC827 cells assessed as induction of EGFR degradation treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis
Protac activity at VHL/EGFR exon 19 deletion mutant in human HCC827 cells assessed as induction of EGFR degradation treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis
[PMID: 31895569]
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]
In Vitro

MS39 (11-point 3-fold dilution series up to 30 μM) binds with high affinity to both purified wild-type EGFR (Kd = 11 nM) and EGFRL858R mutant (Kd = 12 ± 7 nM) proteins in a competitive binding assay[1].
MS39 (1-10000 nM; 16 h) potently induces concentration-dependent degradation of EGFR e19d in HCC-827 cells with a DC50 of 5.0 nM over 16 h, and inhibits downstream EGFR-AKT signaling[1].
MS39 (1-10000 nM; 16 h) potently induces concentration-dependent degradation of EGFRL858R in H3255 cells with a DC50 of 3.3 nM over 16 h, and inhibits downstream EGFR-AKT signaling[1].
MS39 (1-10000 nM; 16 h) does not significantly induce degradation of wild-type EGFR in OVCAR-8 or H1299 cells[1].
MS39 (100-1000 nM; 16 h) has EGFR degradation activity in HCC-827 cells that is enhanced by serum starvation[1].
MS39 (100-1000 nM; 16 h) has EGFR degradation activity in H3255 cells that is enhanced by serum starvation[1].
MS39 (100 nM; 8 h, preceded by 2 h pretreatments with blocking agents) induces EGFR degradation in H3255 cells that is mediated via the VHL E3 ubiquitin ligase pathway and requires EGFR binding[1].
MS39 (100 nM; 12 h treatment, followed by 0-48 h post-washout analysis) induces EGFR degradation and downstream signaling inhibition in HCC-827 cells that are reversible after compound washout[1].
MS39 (100 nM; 12 h treatment, followed by 0-48 h post-washout analysis) induces EGFR degradation and downstream signaling inhibition in H3255 cells that are reversible after compound washout, with slightly prolonged effects relative to HCC-827 cells[1].
MS39 (serial dilution series; 3 days) inhibits the proliferation of H3255 lung cancer cells, with potency greater than its non-functional control MS39N and the EGFR degrader PROTAC3[1].

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

MS39 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCC-827 lung cancer cells (expressing EGFR with exon 19 deletion, EGFR e19d)
Concentration: 1-10000 nM
Incubation Time: 16 h
Result: Induced concentration-dependent degradation of EGFR e19d, achieving over 95% maximum degradation at 50 nM.
Reached a half-maximal degradation concentration (DC50) of 5.0 nM.
Showed a slight "hook effect" at 10000 nM.
Potently inhibited EGFR autophosphorylation (p-EGFR) and AKT phosphorylation (p-AKT).

Western Blot Analysis[1]

Cell Line: H3255 lung cancer cells (expressing EGFR L858R mutant)
Concentration: 1-10000 nM
Incubation Time: 16 h
Result: Induced concentration-dependent degradation of EGFR L858R, achieving over 95% maximum degradation at 50 nM.
Reached a half-maximal degradation concentration (DC50) of 3.3 nM.
Showed no "hook effect" at 10000 nM.
Potently inhibited EGFR autophosphorylation (p-EGFR) and AKT phosphorylation (p-AKT).

Western Blot Analysis[1]

Cell Line: OVCAR-8 ovarian cancer cells (expressing wild-type EGFR), H1299 lung cancer cells (expressing wild-type EGFR)
Concentration: 1-10000 nM
Incubation Time: 16 h
Result: Did not significantly reduce WT EGFR protein levels in either cell line.

Western Blot Analysis[1]

Cell Line: HCC-827 lung cancer cells (expressing EGFR e19d)
Concentration: 100 nM
Incubation Time: 0, 1, 2, 4, 8, 12, 24 h
Result: Induced time-dependent degradation of EGFR e19d, reducing EGFR protein levels by ~50% after 4 h.
Achieved near-complete degradation by 12 h, and sustained complete degradation for up to 24 h.
Reached a half-life (t1/2) of EGFR degradation of 4 h.
Showed robust inhibition of p-AKT after 1 h of treatment.

Western Blot Analysis[1]

Cell Line: H3255 lung cancer cells (expressing EGFR L858R mutant)
Concentration: 100 nM
Incubation Time: 0, 1, 2, 4, 8, 12, 24 h
Result: Induced time-dependent degradation of EGFR L858R, reducing EGFR protein levels by ~50% after 4 h.
Achieved near-complete degradation by 12 h, and sustained complete degradation for up to 24 h.
Reached a half-life (t1/2) of EGFR degradation of 4 h.
Showed inhibition of p-AKT in a time-dependent manner.

Western Blot Analysis[1]

Cell Line: HCC-827 lung cancer cells (expressing EGFR e19d)
Concentration: 100 nM, 1000 nM
Incubation Time: 16 h
Result: Showed a more pronounced EGFR degradation effect in serum-free medium compared to medium containing 10% FBS.

Western Blot Analysis[1]

Cell Line: H3255 lung cancer cells (expressing EGFR L858R mutant)
Concentration: 100 nM, 1000 nM
Incubation Time: 16 h
Result: Showed a more pronounced EGFR degradation effect in serum-free medium compared to medium containing 20% FBS.

Western Blot Analysis[1]

Cell Line: H3255 lung cancer cells (expressing EGFR L858R mutant)
Concentration: 100 nM (MS39; 8 h), 2 h pretreatments with blocking agents
Incubation Time: 8 h (MS39 treatment), 2 h (pretreatment with blocking agents)
Result: Induced EGFR degradation that was blocked by pretreatment with MLN4924, VH-298, or gefitinib.

Western Blot Analysis[1]

Cell Line: HCC-827 lung cancer cells (expressing EGFR e19d)
Concentration: 100 nM
Incubation Time: 12 h (treatment), 0, 1, 2, 4, 8, 12, 24, 48 h (post-washout analysis)
Result: Induced EGFR degradation with EGFR protein levels recovering by 24 h post-washout.
Induced inhibition of p-EGFR with recovery by 24 h post-washout.
Induced inhibition of p-AKT with recovery by 48 h post-washout.

Western Blot Analysis[1]

Cell Line: H3255 lung cancer cells (expressing EGFR L858R mutant)
Concentration: 100 nM
Incubation Time: 12 h (treatment), 0, 1, 2, 4, 8, 12, 24, 48 h (post-washout analysis)
Result: Induced EGFR degradation with EGFR protein levels recovering by 24 h post-washout.
Showed slightly prolonged EGFR degradation and autophosphorylation inhibition compared to HCC-827 cells.

Cell Proliferation Assay[1]

Cell Line: H3255 lung cancer cells (expressing EGFR L858R mutant)
Concentration: Serial dilution series
Incubation Time: 3 days
Result: Effectively inhibited H3255 cell proliferation.
Was more potent than its negative control compound 27 (MS39N) and the previously reported EGFR degrader PROTAC3.
In Vivo

MS39 (50 mg/kg; i.p.; single dose) achieves and sustains high plasma concentrations in male Swiss Albino mice, with levels remaining above 1 μM for 24 hours[1].

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

Animal Model: Swiss Albino (male)[1]
Dosage: 50 mg/kg
Administration: i.p.; single dose
Result: Maintained high plasma concentrations (approximately 5 μM) for over 8 hours post-dosing.
Measured approximately 1 μM plasma concentration at 24 hours post-dosing.
Clinical Trial
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

Purity: 99.89%

SDS (252 KB)

COA (247 KB) HNMR (158 KB) RP-HPLC (169 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
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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MS39 Related Classifications

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  • 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:

MS392675490-92-1MS 39MS-39EGFRPROTACsEpidermal growth factor receptorErbB-1HER1VHL E3 ligaseH3255 cellsEGFR e19dnon-small-cell lung cancerEGFR L858R mutantAKTHCC-827 cellsepidermal growth factor receptorSwiss Albino miceInhibitorinhibitorinhibit

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