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HG-7-85-01

CAS No. : 1258391-13-7

MCE 站：HG-7-85-01

产品活性：HG-7-85-01 是一种 Bcr-Abl，PDGFRα，Kit 和 Src 激酶的野生型和看门突变形式的 II 型 ATP 竞争性抑制剂。HG-7-85-01 抑制 T315I 突变型 Bcr-Abl (T315I mutant Bcr-Abl) 激酶，KDR 和 RET，IC₅₀ 为 3 nM，20 nM 和 30 nM，对其他激酶的抑制作用很小或没有抑制作用 (IC₅₀>2 μM)。HG-7-85-01 通过诱导细胞凋亡 (apoptosis) 和抑制细胞周期进程来抑制细胞增殖。

研究领域：Protein Tyrosine Kinase/RTK  |  Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Apoptosis

作用靶点：Bcr-Abl  |  PDGFR  |  c-Kit  |  Src  |  JAK  |  Apoptosis

In Vitro: HG-7-85-01 (0-1 μM; 24 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment leads to G0G1 arrest of BCR-ABL-expressing cells.
HG-7-85-01 (0-1 μM; 72 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment also leads to induction of apoptosis of BCR-ABL-expressing cells.
HG-7-85-01 treatment potently and selectively inhibits the proliferation of 32D- and Ba/F3 cells expressing nonmutant BCR-ABL and the BCR-ABL-T315I gatekeeper mutant. HG-7-85-01 shows higher potency against nonmutant BCR-ABL and BCR-ABL-T315I (IC₅₀ = 0.06-0.14 μM).
HG-7-85-01 inhibits BCR-ABL kinase activity in a concentration-dependent manner, suggesting selective targeting of the BCR-ABL kinase as the mechanism of action of HG-7-85-01.
HG-7-85-01 potently inhibits the proliferation of Ba/F3 cells expressing the Kit-T670I gatekeeper mutation (Ba/F3- Kit-T670I) and Ba/F3 cells expressing TEL/PDGFRβ and no effect on parental Ba/F3 cells. HG-7-85-01 inhibits Kit, PDGFR phosphorylation in a concentration-dependent manner.
The PDGFRα-T674M and PDGFRα-T674I gatekeeper mutant variants are highly responsive to HG-7-85-01 and significant IL-3 rescue.
HG-7-85-01 inhibits the proliferation of Ba/F3 cells transformed with human c-Src (EC₅₀ = 190 nM), T338I Src (EC₅₀ = 290 nM), and T338M Src (EC₅₀ = 150 nM; chicken c-Src numbering). And potently inhibits the proliferation of exon 11 Kit mutant-expressing cells, exon 9 kit mutant-expressing cells are significantly less responsive.

In Vivo: HG-7-85-01 has limited oral bioavailability (BAV % F mouse = 5 %, rat = 19 %), a moderate half life (T_1/2 mouse =1.1 h rat = 5.8 hours), a relative low maximal serum concentration (C_max mouse = 106 ng/mL at 10 mg/kg , rat = 292 ng/mL and 2 mg/kg ) and a relatively high clearance (Cl mouse = 23 ml/min/kg, rat = 13 ml/min/kg) .

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