ARQ 621Eg5 inhibitor CAS# 1095253-39-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1095253-39-6 | SDF | Download SDF |
| PubChem ID | 25110841 | Appearance | Powder |
| Formula | C28H24Cl2FN5O2 | M.Wt | 552.43 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | N-(3-aminopropyl)-N-[(1R)-1-(3-anilino-7-chloro-4-oxoquinazolin-2-yl)but-3-ynyl]-3-chloro-2-fluorobenzamide | ||
| SMILES | C#CCC(C1=NC2=C(C=CC(=C2)Cl)C(=O)N1NC3=CC=CC=C3)N(CCCN)C(=O)C4=C(C(=CC=C4)Cl)F | ||
| Standard InChIKey | UPJSUQWHUVLLNW-XMMPIXPASA-N | ||
| Standard InChI | InChI=1S/C28H24Cl2FN5O2/c1-2-8-24(35(16-7-15-32)27(37)21-11-6-12-22(30)25(21)31)26-33-23-17-18(29)13-14-20(23)28(38)36(26)34-19-9-4-3-5-10-19/h1,3-6,9-14,17,24,34H,7-8,15-16,32H2/t24-/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
ARQ 621 Dilution Calculator
ARQ 621 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8102 mL | 9.0509 mL | 18.1018 mL | 36.2037 mL | 45.2546 mL |
| 5 mM | 0.362 mL | 1.8102 mL | 3.6204 mL | 7.2407 mL | 9.0509 mL |
| 10 mM | 0.181 mL | 0.9051 mL | 1.8102 mL | 3.6204 mL | 4.5255 mL |
| 50 mM | 0.0362 mL | 0.181 mL | 0.362 mL | 0.7241 mL | 0.9051 mL |
| 100 mM | 0.0181 mL | 0.0905 mL | 0.181 mL | 0.362 mL | 0.4525 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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ARQ 621 is a novel, allosteric, potent and selective inhibitor of Eg5. Eg5 is a member of the mitotic kinesin 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 t1/2 value 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]. IC50 value of ARQ 621 for CYP 1A2, 2C9, 2D6, 3A4, 2C19, and 2C8 was >20, >20, >20, 4.1, 4.0, and 15 ?M, 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 280 mg/m2[2,3].
References:
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.
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.
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.
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