Nilotinib monohydrochloride monohydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服的天然和突变 Bcr-Abl 抑制剂，IC50 为 20-80 nM。

A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM; inhibits proliferation of Ba/F3 cells expressing G250E, E255K(V), F317L, M351T, F486S, M244V, L248R, Q252H, Y253H, E255K, E279K, E282D, V289S, and L348M Bcr-Abl mutants at <1 uM; also inhibits activated forms of PDGFR and c-Kit with IC50 of 30-200 nM; prolongs survival of mice with leukemia due to imatinib-resistant mutants of Bcr-Abl.Blood Cancer Approved(In Vitro):Nilotinib (AMN107) monohydrochloride monohydrate, selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC50<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance.Nilotinib monohydrochloride monohydrate demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC50 of 4.59±0.97 μM and 11.15±1.48 μM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC50 values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively.(In Vivo):Nilotinib monohydrochloride monohydrate (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft.Nilotinib monohydrochloride monohydrate has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon.

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Animal Model:BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X) Dosage:40 mg/kg Administration:Oral gavage; daily; 4 weeks Result:Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.

AMN-107 | AMN107 | Tasigna

Angiogenesis

Bcr-Abl

Bcr-Abl

Cancer

Blood cancer

923288-90-8

583.992

C28H25ClF3N7O2

>98% (HPLC)

DMSO: ≥ 33 mg/mL

CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5.O.Cl

Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-, hydrochloride, hydrate (1:1:1)

(-20℃)

With Ice Pack

≥ 2 years