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ARQ 621 Sale

目录号 : GC16472

An Eg5 inhibitor

ARQ 621 Chemical Structure

Cas No.:1095253-39-6

规格 价格 库存 购买数量
5mg
¥1,050.00
现货
25mg
¥3,518.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

ARQ 621 is a novel, allosteric,potent and selective inhibitor of Eg5. Eg5 is a member of the mitotickinesin superfamily which plays a key role in mitosis. Eg5 is essential for the dynamic organization of the mitotic spindle. Over-expression of Eg5 leads to genomic instability and tumor formation [1].

In vitro: In human liver microsomes, t1/2 of ARQ 621 was 53 min. The t1/2value of ARQ 621 in male and female mouse, rat, dog and monkey liver microsomes was 43, 53, 56, 53, 47, 44, 36, and 32 minutes, respectively [1]. IC50value of ARQ 621 for CYP 1A2, 2C9, 2D6, 3A4, 2C19, and 2C8 was>20, >20, >20, 4.1, 4.0, and 15 µM, respectively. ARQ 621 showed anti-tumor activity with potencies in the low nanomolar range across a range of human solid and hematological malignanciescancer cell types such as colon, NSCLC, gastric, and hematologic cancer cell lines [1].

In vivo: Oral administration of ARQ 621 showed that the bioavailability of ARQ 621 was approximately 9% [1].

Clinical trial: ARQ 621 was currently being tested in a Phase I clinical trial in cancer patients. ARQ 621 (10 mg/m2/week) was administered weekly intravenously over 1-2 hours. Adverse events emerged in 95.9% patients. The main drug-related side-effects were fatigue, acute intravascular hemolysis, and abdominal pain. ARQ 621 appeared to be well tolerated at the weekly dose of 280mg/m2[2,3].

References:
[1].Savage R E, Zhong C, Hall T, et al.  In vitro ADME properties of ARQ 621: A specific Eg5 inhibitor[J]. Cancer Research, 2010, 70(8 Supplement): 5783-5783.
[2].Rosen L, Chen L C, Iyengar T, et al.  ARQ 621, a novel potent and selective inhibitor of Eg5: preclinical data and early results from a clinical phase 1 study[J]. Cancer Research, 2010, 70(8 Supplement): 2750-2750.
[3.Chen L C, Rosen L S, Iyengar T, et al.  First-in-human study with ARQ 621, a novel inhibitor of Eg5: Final results from the solid tumors cohort[C]//ASCO Annual Meeting Proceedings. 2011, 29(15_suppl): 3076.

Chemical Properties

Cas No. 1095253-39-6 SDF
化学名 (R)-N-(3-aminopropyl)-3-chloro-N-(1-(7-chloro-4-oxo-3-(phenylamino)-3,4-dihydroquinazolin-2-yl)but-3-yn-1-yl)-2-fluorobenzamide
Canonical SMILES C#CC[C@](N(C(C1=C(F)C(Cl)=CC=C1)=O)CCCN)([H])C(N2NC3=CC=CC=C3)=NC4=C(C2=O)C=CC(Cl)=C4
分子式 C28H24Cl2FN5O2 分子量 552.43
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8102 mL 9.0509 mL 18.1018 mL
5 mM 0.362 mL 1.8102 mL 3.6204 mL
10 mM 0.181 mL 0.9051 mL 1.8102 mL
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