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Nilotinib monohydrochloride monohydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nilotinib monohydrochloride monohydrate图片
CAS NO:923288-90-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议
5 g电议

产品名称
尼洛替尼盐酸盐一水合物
AMN107 monohydrochloride monohydrate
产品介绍
Nilotinib monohydrochloride monohydrate 是一种二代酪氨酸酶抑制剂,有效抑制BCR-ABL及其突变体。
生物活性

Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent againstBCR-ABL, and is active against manyBCR-ABLmutants.

IC50& Target

Bcr-Abl[1]

体外研究
(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[1].
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 IC50of 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 IC50values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively[2].

体内研究
(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[2].
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[3].

Animal Model:BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2]
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.
Clinical Trial
分子量

583.99

性状

Solid

Formula

C28H25ClF3N7O2

CAS 号

923288-90-8

中文名称

尼洛替尼盐酸盐一水合物;尼罗替尼盐酸盐一水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 33 mg/mL(56.51 mM)

H2O :< 0.1 mg/mL (ultrasonic)(insoluble)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7124 mL8.5618 mL17.1236 mL
5 mM0.3425 mL1.7124 mL3.4247 mL
10 mM0.1712 mL0.8562 mL1.7124 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。