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ChemicalBook >> CAS DataBase List >>4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)-

4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)-

CAS No.
2378188-21-5
Chemical Name:
4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)-
Synonyms
EGFR/C797S-IN-1;4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)-
CBNumber:
CB313035445
Molecular Formula:
C28H30N4O3
Molecular Weight:
470.56
MDL Number:
MOL File:
2378188-21-5.mol
Last updated:2025-04-28 21:36:36

4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)- Properties

Boiling point 607.9±55.0 °C(Predicted)
Density 1.212±0.06 g/cm3(Predicted)
pka 8.92±0.10(Predicted)

4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)- Chemical Properties,Uses,Production

Uses

EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 μM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner[1].

in vivo

EGFR/C797S-IN-1 (10, 30 mg/kg; daily for 14 days) significantly decreases tumor growth in a dose-dependent manner in mouse[1].
Pharmacokinetic Parameters of EGFR/C797S-IN-1 in Male Sprague-Dawley rats[1].

Parameteri.v. (1 mg/kg)p.o. (10 mg/kg)
Tmax (h)0.08±03.33±1.15
T1/2 (h)1.97±0.143.89±0.42
Cmax (ng/mL)69.57±6.787.43±1.17
AUC0-t (h*ng/mL)65.48±5.5561.12±6.23
AUC0-∞ (h*ng/mL)67.98±5.5662.15±6.36
CL-obs (L/h/kg)14.78±1.19--
Vss-obs (L/kg)26.11±2.58--
F (%)--9.33±0.95
Male Sprague-Dawley rats, 1 mg/kg iv ; 10 mg/kg po (dissolved in 5% DMSO, 10% Solutol and 85% Salinet with the concentration of 0.2 mg/mL for i.v. and 1 mg/mL for p.o.)[1].
Animal Model:SD male rats[1]
Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o.
Administration:i.v. or p.o.
Result:Displayed good biochemical activity and promising cellular activity.
Animal Model:BALB/c nude mice (BaF3-EGFR19del/T790M/C797S xenograft model)[1]
Dosage:10, 30 mg/kg
Administration:I.p.; daily for 14 days
Result:Displayed an obvious suppressive effect of tumor growth, with the TGI at 51.36% and 67.95% at the dosage of 10 mg/kg and 30 mg/kg, respectively.

IC 50

EGFRL858R/T790M/C797S: 0.128 μM (IC50)

References

[1] Dou D, et al. Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors. Eur J Med Chem. 2022 Dec 15;244:114856. DOI:10.1016/j.ejmech.2022.114856

4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)- Preparation Products And Raw materials

Raw materials

Preparation Products

4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)- Suppliers

Global( 2)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc. 		+17819995354 marketing@targetmol.com United States 19904 58
TargetMol Chemicals Inc. 15002134094 marketing@targetmol.cn China 21356 58

View Lastest Price from 4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)- manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
EGFR/C797S-IN-1 pictures 2025-04-27 EGFR/C797S-IN-1
2378188-21-5
 US $1520.00-2500.00 / mg 10g TargetMol Chemicals Inc.
  • EGFR/C797S-IN-1 pictures
  • EGFR/C797S-IN-1
    2378188-21-5
  • US $1520.00-2500.00 / mg
  • TargetMol Chemicals Inc.
4-Quinazolinamine, 6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-N-(4-phenoxyphenyl)- EGFR/C797S-IN-1 2378188-21-5