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Art. -Nr.: HY-178057

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EGFR-IN-176

EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR^{19del/T790M/C797S} and EGFR^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2754394-10-8
Formel: C₃₅H₄₅N₁₁O₃S
Molecular Weight:699.87

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

EGFR-IN-176 Chemical Structure

CAS. Nr.: 2754394-10-8

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

In Vitro

EGFR-IN-176 (Compound 31r, 0.0045 nM-10,000 nM, 48 h) exhibits extremely potent and selective growth inhibitory activity against cells harboring EGFR triple mutation in vitro, including Ba/F3 EGFR^{19del/T790M/C797S} (IC₅₀ = 0.001 nM) and Ba/F3 EGFR^{L858R/T790M/C797S} (IC₅₀ = 0.04 nM), with low cytotoxicity towards wild-type EGFR cells A431 (IC₅₀ > 10,000 nM)^[1].
EGFR-IN-176 (500 nM, 7 days) inhibits PC-9 EGFR^{19del/T790M/C797S} and PC-9 EGFR^{L858R/T790M/C797S} proliferation in the short term and deprives cancer cells of their self-renewal and clonogenic growth capabilities in the long term^[1].
EGFR-IN-176 (250 nM, 0-24 h) can effectively inhibit the migration ability of PC-9 EGFR^{19del/T790M/C797S} and PC-9 EGFR^{L858R/T790M/C797S}^[1].
EGFR-IN-176 (500 nM, 48 h) can induce PC-9 EGFR^{19del/T790M/C797S} and PC-9 EGFR^{L858R/T790M/C797S} apoptosis^[1].

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3 EGFR^{19del/T790M/C797S} and Ba/F3 EGFR^{L858R/T790M/C797S}
Concentration:

0.0045 nM ~ 10,000 nM
Incubation Time:

48 h
Result:

Exhibited higher activity, with IC₅₀ values of 0.001 nM (Ba/F3 EGFR^{19del/T790M/C797S}) and 0.04 nM (Ba/F3 EGFR^{L858R/T790M/C797S}).

Cell Migration Assay ^[1]

Cell Line:

PC-9 EGFR^{19del/T790M/C797S} and PC-9 EGFR^{L858R/T790M/C797S}
Concentration:

250 nM
Incubation Time:

24 h
Result:

Significantly slowed down the healing rate of scratches.

Apoptosis Analysis^[1]

Cell Line:

PC-9 EGFR^{19del/T790M/C797S} and PC-9 EGFR^{L858R/T790M/C797S}
Concentration:

500 nM
Incubation Time:

48 h
Result:

significantly increased the proportion of early and late apoptotic cells

Parmacokinetics

Species	Dose	Route	AUC_0-t	T_1/2	V_ss	CL	C_max	F	T_max
Rat^[1]	1 mg/kg	i.v.	1720 ng·h/mL	8.6 h	6.1 L/kg	8.8 mL/min/kg	/	/	/
Rat^[1]	10 mg/kg	i.g.	/	/	/	/	323 ng/mL	23.5 %	4 h

In Vivo

EGFR-IN-176 (Compound 31r) (40-80 mg/kg, i.g., once daily for 21 days) can dose-dependently significantly inhibit or even promote tumor regression in PC-9 xenograft mice^[1].

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

Animal Model:

Subcutaneously inoculate the right forelimb of 6-8-week-old BALB/c-nu mice with a 0.2 mL suspension of PC-9 EGFR^{19del/T790M/C797S} cells at a concentration of 2.5×10^7 cells/mL until the tumor volume reaches 100-200 cubic millimeters.
Dosage:

40 mg/kg, 60 mg/kg, 80 mg/kg
Administration:

Oral gavage, once daily for 21 days
Result:

Showed a dose-dependent tumor growth inhibitory effect, the tumor growth inhibition rates (TGI) were 80.2% (40 mg/kg), 92.3% (60 mg/kg), and 105.7% (80 mg/kg), respectively.
Observed tumor regression in the high-dose group (80 mg/kg), the tumor volume decreased to below the initial volume.
Exhibited favorable in vivo tolerability, with no mortality or significant body weight loss observed.
Significantly inhibited EGFR phosphorylation and the activation of downstream signaling pathways.

Chemical Information

CAS. Nr. 2754394-10-8
Molecular Weight 699.87
Formel C₃₅H₄₅N₁₁O₃S
SMILES

O=S(N(C)C1=C2N=CC=NC2=CC=C1NC3=C4C=CNC4=NC(NC5=C(OC)C=C(N6CCC(CC6)N7CCN(CC7)C)C(CC)=C5)=N3)(C)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)
Handling Instructions (2659 KB)

Verweise

[1]. Wu Z, et al. Discovery of Potent and Selective Pyrrolo[2,3-d]pyrimidine Derivatives as Fourth-Generation EGFR Inhibitors Targeting Triple Mutation. J Med Chem. 2025 Sep 25;68(18):19205-19228. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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