ARQ 621 Chemical Structure

ARQ 621 Chemical Structure
Molecular Weight: 552.43

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.
Targets Eg5 mitotic motor protein [1]
In vitro ARQ 621 demonstrates anti-tumor activity against a wide range of human cancer cell lines in vitro, including colon, lung, endometrial, bladder, and hematologic cancer cell lines, with significantly less cytotoxicity against hematopoietic cells. [1]
In vivo ARQ 621, as a novel clinical stage drug candidate, inhibits a number of xenografts grown in athymic mice, such as pancreatic, breast, prostate, and ovarian carcinomas with no hematological changes. Furthermore, for ARQ 621, there is no envidence of bone marrow toxicity in pre-clinical mouse efficacy models or safety studies in rats and dogs. [1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rosen L, et al. Annual Meeting of ASCO: abstract 3076

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00825487 Completed Metastatic Solid Tumors, Refractory/Relapsed Hematologic Malignancies ArQule August 2009 Phase 1

Chemical Information

Download ARQ 621 SDF
Molecular Weight (MW) 552.43
Formula

C28H24Cl2FN5O2

CAS No. 1095253-39-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (181.01 mM)
Ethanol 100 mg/mL (181.01 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(3-aminopropyl)-3-chloro-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylamino)-2-quinazolinyl]-3-butyn-1-yl]-2-fluoro-benzamide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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