| Identification | Back Directory | [Name]
N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide | [CAS]
1557267-42-1 | [Synonyms]
CS-2348
Avitinib
Avi Tini
Abivertinib
Avitinib (AC0010)
Avitinib free base
Avitinib(AC0010/AC0010MA)
N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide
2-Propenamide, N-[3-[[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]- | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C26H26FN7O2 | [MDL Number]
MFCD29089376 | [MOL File]
1557267-42-1.mol | [Molecular Weight]
487.53 |
| Chemical Properties | Back Directory | [density ]
1.365±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:30.0(Max Conc. mg/mL);61.53(Max Conc. mM) | [form ]
A crystalline solid | [pka]
12.48±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.1 In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.1 | [Uses]
Abivertinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). Abivertinib synergistically strengthens anti-leukemia activity of venetoclax in acute myeloid leukemia in BTK-dependent manner. | [in vivo]
Avitinib (AC0010; 12.5-500 mg/kg; orally administration; once daily; for 14 days) inhibits EGFR-mutant tumor growth but not wild-type EGFR tumor growth in xenograft models over extended duration[1]. | Animal Model: | Nu/Nu nude mice (Six- to 8-week-old) injected with NCI-H1975 and A431 cells[1] | | Dosage: | 12.5, 50, and 500 mg/kg | | Administration: | Orally administration; once daily; for 14 days | | Result: | Inhibited EGFR-mutant tumor growth but not wild-type EGFR tumor growth. |
| [IC 50]
EGFR L858R: 0.18 nM (IC50); EGFRT790M: 0.18 nM (IC50); EGFR (WT): 7.68 nM (IC50) | [storage]
Store at -20°C |
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