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Ilginatinib hydrochloride

CAS No. : 1239358-85-0

MCE 站：Ilginatinib hydrochloride

产品活性：Ilginatinib hydrochloride (NS-018 hydrochloride) 是一种高度有效的，可口服的 JAK2 抑制剂，IC₅₀ 值为 0.72 nM，对其选择性是对 JAK1 的 46 倍 (IC₅₀, 33 nM)，JAK3 的 54 倍 (IC₅₀, 39 nM)，以及 Tyk2 的 22 倍 (IC₅₀, 22 nM)。

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

作用靶点：JAK

In Vitro: Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active JAK2 inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM). Ilginatinib hydrochloride also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. Ilginatinib hydrochloride shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC₅₀ of 11-120?nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2.
Ilginatinib hydrochloride (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). Ilginatinib hydrochloride (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients.

In Vivo: Ilginatinib hydrochloride (NS-018 hydrochloride) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model.
Ilginatinib hydrochloride (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  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  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AG490  |  Upadacitinib  |  AT9283  |  Gandotinib  |  Lestaurtinib  |  Cucurbitacin I  |  Oclacitinib maleate  |  JANEX-1  |  XL019  |  Atractylenolide I  |  FLLL32  |  LFM-A13  |  Brevilin A  |  ZM39923 hydrochloride  |  Ginsenoside Rk1  |  WHI-P154  |  Curculigoside  |  FM-381  |  RO8191  |  Reticuline  |  TCS 21311  |  WHI-P97  |  Coumermycin A1  |  Delphinidin chloride  |  Ilginatinib maleate  |  Protosappanin A  |  Dehydrocrenatidine  |  FM-479  |  NSC 33994

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