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Nilotinib(AMN-107) Sale

(Synonyms: 尼洛替尼; AMN107) 目录号 : GC14129

A Bcr-Abl inhibitor

Nilotinib(AMN-107) Chemical Structure

Cas No.:641571-10-0

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100mg
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment: [1]

Cell lines

CD34+ cells from individual patients with CML

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

5 μM, 16 hours

Applications

After 16 hours in culture with nilotinib, long enough for inhibition of CrkL phosphorylation but not for induction of apoptosis, the total CD34+ cell samples studied exhibited only partial and variable inhibition (range, 49% to 0% inhibition) of CrkL phosphorylation.

Animal experiment: [2]

Animal models

C57Bl/6J mice injected with 8093 lymphoma cells

Dosage form

Oral administration, 75 mg/kg, daily

Applications

Vehicle treated mice became moribund within 3 weeks of the transplantation. They showed clear symptoms of ALL. Nilotinib-treated mice lived statistically significantly longer as compared with the vehicle-treated mice. This result clearly indicated that nilotinib was very effective in inhibiting the proliferation of the leukemic cells in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Jørgensen H G, Allan E K, Jordanides N E, et al. Nilotinib exerts equipotent antiproliferative effects to imatinib and does not induce apoptosis in CD34+ CML cells. Blood, 2007, 109(9): 4016-4019.

[2] Kaur P, Feldhahn N, Zhang B, et al. Nilotinib treatment in mouse models of P190 Bcr/Abl lymphoblastic leukemia. Mol Cancer, 2007, 6(10): 67-77.

产品描述

Nilotinib is a selective, oral inhibitor of tyrosine kinase with IC50 values of 20, 42, 31, 38, 29 and 41 nM for the autophosphorylation of native BCR-ABL (WT p210) and mutant BCR-ABL (E281K, E292K, F317L, M351T and F486S), respectively [1].

Nilotinib was designed based on the structure of imatinib and showed the superiority over imatinib in newly diagnosed or imatinib-resistant chronic myelogenous leukemia (CML). It was more potent than imatinib to wild-type BCR-ABL in a wide range of CML-derived and transfected cell lines. Nilotinib was also efficacious in gastrointestinal stromal tumors. Nilotinib showed inhibition activities in KIT mutant cells, including KITV560del, KITK642E and KITV560G (IC50 value of 108 nM). It also was effect to double mutations of KIT, such as KITV560del/V654A, KITV559D/D820Y, KITV560del/V654A (IC50: 192 nM) and KITV559D/D820Y (IC50: 297 nM). Besides that, Nilotinib exerted selective inhibition of PDGFRα and PDGFRβ. It suppressed cell proliferation with IC50 value of 0.54 nM in EOL-1 cells with constitutive activation of FIP1L1-PDGFRα [1, 2].

References:
[1] Weisberg E, Manley P, Mestan J, et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. British Journal of Cancer, 2006, 94(12): 1765-1769.
[2] Blay J Y, Von Mehren M. Nilotinib: a novel, selective tyrosine kinase inhibitor//Seminars in oncology. WB Saunders, 2011, 38: S3-S9.

Chemical Properties

Cas No. 641571-10-0 SDF
别名 尼洛替尼; AMN107
化学名 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
Canonical SMILES CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)N3C=C(N=C3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5
分子式 C28H22F3N7O 分子量 529.53
溶解度 ≥ 26.5mg/mL in DMSO, ≥ 5mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
General tips 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8885 mL 9.4423 mL 18.8847 mL
5 mM 0.3777 mL 1.8885 mL 3.7769 mL
10 mM 0.1888 mL 0.9442 mL 1.8885 mL
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