| Identification | Back Directory | [Name]
EGFR-IN-7 (compound 34) | [CAS]
2267329-76-8 | [Synonyms]
TBQ3804
TQB3804
EGFR-IN-7
EGFR Inhibitor 2
Egfr-IN-7(TQB3804 )
EGFR-IN-7 (COMPOUND 34)
2,4-Pyrimidinediamine, 5-bromo-N4-[5-(dimethylphosphinyl)-6-quinoxalinyl]-N2-[2-methoxy-5-methyl-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]- | [Molecular Formula]
C32H41BrN9O2P | [MDL Number]
MFCD32689509 | [MOL File]
2267329-76-8.mol | [Molecular Weight]
694.6 |
| Chemical Properties | Back Directory | [Boiling point ]
858.7±75.0 °C(Predicted) | [density ]
1.44±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCL and heat to 60°C) | [form ]
Solid | [pka]
8.14±0.42(Predicted) | [color ]
Light yellow to yellow | [InChIKey]
ZYSKXRAGBGLELB-UHFFFAOYSA-N | [SMILES]
C1(NC2=CC(C)=C(N3CCC(N4CCN(C)CC4)CC3)C=C2OC)=NC=C(Br)C(NC2=CC=C3C(=C2P(C)(C)=O)N=CC=N3)=N1 |
| Hazard Information | Back Directory | [Uses]
EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers[1]. | [in vivo]
EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o.; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model[1].
EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model[1]. | Animal Model: | Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)[1] | | Dosage: | 5, 15, 45 mg/kg | | Administration: | Oral administration, daily, for 13 days | | Result: | Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice. |
| Animal Model: | Subcutaneous xenograft PC-9 (Δ19del) model[1] | | Dosage: | 0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg | | Administration: | Oral administration, once a day, 3 weeks | | Result: | Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy. |
| [IC 50]
EGFR (WT): 7.92 nM (IC50); EGFR (C797S/T790M/L858R): 0.218 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Ling WY, et, al. Prostaglandin E2 suppresses bacterial killing in alveolar macrophages by inhibiting NADPH oxidase. WO2019015655A1. |
|
| Company Name: |
RuiKeXin Gold
|
| Tel: |
19938953786 |
| Website: |
ahreaction.com/ |
| Company Name: |
Twochem Co.Ltd
|
| Tel: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
|