Products

Enzymes for Research, Diagnostic and Industrial Use

Products
Online Inquiry

Our Products Cannot Be Used As Medicines Directly For Personal Use.

24 hour
Promise

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

ARRY 520 trifluoroacetate

Cat No.
CEI-1218
Product Overview
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. 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.
CAS No.
885060-09-3
Molecular Weight
420.48
Purity
0.98
Storage
Store at -20°C
Targets
KSP
Molecular Formula
C20H22F2N4O2S. CF3CO2H
Chemical Name
(2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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.
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.

Our Products Cannot Be Used As Medicines Directly For Personal Use.

0
Click unfold / close
Inquiry Basket
Delete selected Quote Check Out
Decide to move out of the shopping cart?
Sure No, Back

Please choose product!

< Go Back
You have already added to buy this product