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Varlitinib tosylate

CAS No. : 1146629-86-8

MCE 站：Varlitinib tosylate

产品活性：Varlitinib (ASLAN001) tosylate 是有效，可逆的泛 EGFR 小分子抑制剂，对 HER1，HER2 和 HER4 的 IC₅₀ 值分别为7，2，4 nM。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib tosylate (ARRY-334543) potently inhibits substrate phosphorylation. Varlitinib tosylate is shown to be highly selective for EGFR/ErbB-2, ａnd does not show any significant activity when screened against a panel of 104 kinases.

In Vivo: Varlitinib tosylate treatment potently inhibits tumor growth with complete tumor regression observed at dosing of 100 mg/kg twice a day. After five days of Varlitinib tosylate treatment, phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal, 4EBP1, Cdk-2, Cdc-2 ａnd retinoblastoma are strongly inhibited. Varlitinib tosylate treatment results in a significant reduction in survivin ａnd a concomittant increase in Caspase 3 cleavage products. In murine xenograft models, Varlitinib tosylate (ARRY-334543) demonstrates significant dose-related (25, 50, 100 mg/kg) tumor growth inhibition in A431-derived tumors when administered orally, twice a day, for 21 days.

相关产品：EGFR/HER2/CDK9-IN-2  |  Lapatinib ditosylate  |  BMS-690514  |  Erlotinib-d₆ (hydrochloride)  |  EGFR/CDK2-IN-1  |  JBJ-04-125-02  |  EGFR-IN-22  |  EGFR-IN-34  |  Epertinib  |  Ponezumab  |  Erlotinib Hydrochloride  |  EGFR-IN-36  |  EGFR-IN-62  |  Genistein  |  Panitumumab (anti-EGFR)  |  Lirafugratinib  |  Lapatinib-d₇ (dihydrochloride)  |  (E/Z)-CP-724714  |  TAS0728  |  Rezivertinib  |  Tucatinib hemiethanolate  |  Osimertinib mesylate  |  AV-412 free base  |  Falnidamol  |  EGFR/ErbB-2/ErbB-4 inhibitor-2  |  Trastuzumab  |  EGFR-IN-58  |  Naquotinib  |  MS9449

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