ARRY 520 trifluoroacetate
(Synonyms: ARRY-520) 目录号 : GC11656
A potent Eg5 inhibitor
Cas No.:885060-09-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ARRY 520 trifluoroacetate is a synthetic and salt form of KSP inhibitor with IC50 value of 6 nM.
Kinesin spindle protein (KSP) is one member of the mitotic kinesins involved in the early stages of mitosis responsible for centrosome separation.
In vitro: ARRY-520 had low nanomolar antiproliferative activity in various tumor cell lines and exhibited activity in multidrug-resistant cell lines. EC50s of ARRY-520 for proliferation inhibition in HCT-15, NCI/ADR-RES and K562/ADR cells was 3.7, 14 and 4.2 nM, respectively, while paclitaxel EC50s in these cell lines was 35, 565 and 372 nM. Moreover, K562/ADR was found to be 118-fold resistant to paclitaxel when compared to the parent K562 line, but only 3.5-fold resistant to that of ARRY-520 [1].
In vivo: ARRY-520 was found to be active in UISO-BCA-1 xenografts, which were completely resistant to paclitaxel. The antitumor efficacy of ARRY-520 was also found to be superior to paclitaxel in mice bearing HT-29, HCT-116, MDA-MB-231 and A2780 xenografts. ARRY-520 was superior to docetaxel in the androgen receptor-negative prostate cancer PC-3 xenograft model, and was also superior to docetaxel in the DU145 prostate xenograft model [1].
Clinical trial: A phase I trial was conducted to establish the safety and the maximum tolerated dose (MTD) of ARRY-520. The MTD was 4.5 mg/m2 total dose per cycle for both dose schedules. Dose-limiting toxicities included exfoliative rash, hand-foot-syndrome, mucositis, and hyperbilirubinemia. Grades 3 or 4 reversible drug-related myelosuppression were observed in 33 of 36 patients [2].
References:
[1] Woessner R, Tunquist B, Lemieux C, Chlipala E, Jackinsky S, Dewolf W Jr, Voegtli W, Cox A, Rana S, Lee P, Walker D. ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Anticancer Res. 2009;29(11):4373-80.
[2] Khoury HJ, Garcia-Manero G, Borthakur G, Kadia T, Foudray MC, Arellano M, Langston A, Bethelmie-Bryan B, Rush S, Litwiler K, Karan S, Simmons H, Marcus AI, Ptaszynski M, Kantarjian H. A phase 1 dose-escalation study of ARRY-520, a kinesin spindle protein inhibitor, in patients with advanced myeloid leukemias. Cancer. 2012;118(14):3556-64.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3782 mL | 11.8912 mL | 23.7823 mL |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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