Cat. No.: HY-157581

MS39

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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: VHL ligand (HY-125845); Black: linker (HY-W014125)).

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Pureté: 99.89%
CAS No.: 2675490-92-1
Formule: C₅₅H₇₁ClFN₉O₇S
Masse moléculaire:1056.72

Stockage:

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

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

MS39 Chemical Structure

CAS No.: 2675490-92-1

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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: VHL ligand (HY-125845); Black: linker (HY-W014125)).

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform PROTACs :

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 (K_d=11 nM) and EGFR^L858R mutant (K_d=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 EGFR^L858R in H3255 cells with a DC₅₀ of 3.3 nM over 16 h, and inhibits downstream EGFR-AKT signaling^[1].

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

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2675490-92-1
Appearance Solid
Masse moléculaire 1056.72
Formule C₅₅H₇₁ClFN₉O₇S
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9463 mL

4.7316 mL

9.4632 mL

5 mM

0.1893 mL

0.9463 mL

1.8926 mL

10 mM

0.0946 mL

0.4732 mL

0.9463 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (252 KB)
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- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Cheng M, et al. Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. J Med Chem. 2020;63(3):1216-1232. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MS39

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MS39 Related Classifications

HY-157581 Related Classifications