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CG-806

CAS No. : 1370466-81-1

MCE 站：CG-806

产品活性：CG-806 是一种口服，有效且非共价的泛-FLT3/泛-BTK 抑制剂，对 FLT3 的 IC₅₀ 值为 0.08 µM。CG-806 对 FLT3 野生型转染的 Ba/F3 细胞的 IC₅₀ 值为 11 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FLT3  |  Btk

In Vitro: In FLT3-ITD AML cells, CG-806 induces apoptosis through inhibition of FLT3 signaling (decreases phospho-FLT3, -STAT5 ａnd -ERK) ａnd promotion of G0/G1 cell cycle arrest. In FLT3-WT AML cell lines, or Ba/F3 cells transfected with FLT3-WT, D835Y, ITD+D835Y, or ITD+F691L, CG-806 markedly decreases phosphorylation of BTK, aurora kinases (AURK) ａnd H3S10, resulting in G2/M arrest or polyploidy, ａnd apoptosis with less or no effect on FLT3-WT activity. CG-806 decreases BTK phosphorylation in all malignant B cell lines tested ａnd inhibits cell proliferation ａnd colony formation.CG-806 equivalently inhibits BTK-WT ａnd BTK-C481S in HEK293 transfected cells.

In Vivo: CG-806 (0-120 mg/kg; oral administration; for 28 days; CD-1 mice) treatment suppresses leukemia growth at all doses tested throughout the 28-day period of dosing, ａnd has no adverse CG-806-related effects on body weight, ophthalmic, respiratory or neurological examinations, clinical pathology (coagulation, clinical chemistry, or urinalysis), organ weight or macroscopic evaluations in the subcutaneous MV4-11 xenograft model.

相关产品：Covalent Screening Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Covalent Screening Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  AT9283  |  Gandotinib  |  KW-2449  |  Lestaurtinib  |  Ibrutinib-biotin  |  AST 487  |  LFM-A13  |  Ibrutinib deacryloylpiperidine  |  JNJ-47117096 hydrochloride  |  PCI 29732  |  BPR1J-097 Hydrochloride  |  Crotonoside  |  Tyrphostin AG1296  |  SKLB4771  |  Acalabrutinib D4  |  TCS 359  |  3-Hydroxy Midostaurin  |  Hypothemycin  |  Sorafenib (D3)  |  (R)-3-Hydroxy Midostaurin  |  (S)-3-Hydroxy Midostaurin  |  5＇-Fluoroindirubinoxime  |  BPR1K871

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