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Altiratinib

CAS No. : 1345847-93-9

MCE 站：Altiratinib

产品活性：Altiratinib (DCC-2701) 是多靶点激酶抑制剂，抑制 MET，TIE2，VEGFR2，FLT3，Trk1，Trk2 和 Trk3 的 IC₅₀ 值分别为2.7，8，9.2，9.3，0.85，4.6，0.83 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Neuronal Signaling

作用靶点：VEGFR  |  c-Met/HGFR  |  FLT3  |  Trk Receptor

In Vitro: Altiratinib also inhibits MET isoforms MET^D1228H, MET ^D1228N, MET^Y1230C, MET^Y1230D, MET^Y1230H, MET^M1250T with IC₅₀s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC₅₀ values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC₅₀=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC₅₀ of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC₅₀ of 12 nM.

In Vivo: A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood–brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases.

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