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CHZ868

CAS No. : 1895895-38-1

MCE 站：CHZ868

产品活性：CHZ868是类型II的JAK2抑制剂，抑制EPOR JAK2 WT Ba/F3 cell细胞的IC₅₀值为0.17 μM。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：JAK

In Vitro: CHZ868 potently inhibits constitutive JAK2 ａnd STAT5 phosphorylation in JAK2V617F SET2 cells. CHZ868 potently inhibits the proliferation of SET2 cells (GI₅₀=59nM), ａnd has 6-fold less growth inhibitory activity against CMK cells (GI₅₀=378nM). At 100 nM CHZ868 has activity against 26 kinases, including JAK2 ａnd TYK2. CHZ868 is thought to engage with the hinge region of JAK2 through two H-bonds, formed between the amino-pyridine of CHZ868 ａnd the backbone-NH/CO of L932, while the pyridine is occupying the adenine pocket of the ATP binding site. CHZ868 potently suppresses the growth of CRLF2-rearranged human B-ALL cells, abrogates JAK2 signaling.

In Vivo: CHZ868 is characterized by high passive permeability, good metabolic stability, ａnd low water solubility, as well as by moderate blood clearance ａnd good oral bioavailability, making it suitable for in vivo use. CHZ868 improves survival in mice with human or murine B-ALL. CHZ868 ａnd dexamethasone synergistically induces apoptosis in JAK2-dependent B-ALLs ａnd further improves survival compared to CHZ868 alone.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AG490  |  Upadacitinib  |  AT9283  |  Gandotinib  |  Lestaurtinib  |  Oclacitinib maleate  |  JANEX-1  |  Cucurbitacin I  |  XL019  |  Atractylenolide I  |  FLLL32  |  Brevilin A  |  LFM-A13  |  Ginsenoside Rk1  |  ZM39923 hydrochloride  |  WHI-P154  |  Curculigoside  |  FM-381  |  RO8191  |  Reticuline  |  Ilginatinib maleate  |  TCS 21311  |  WHI-P97  |  Protosappanin A  |  Coumermycin A1  |  Dehydrocrenatidine  |  Delphinidin chloride  |  FM-479  |  NSC 33994

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