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CC-671

Catalog No. T4482   CAS 1618658-88-0

CC-671 is a dual TTK protein kinase (IC50: 0.005 μM) /CLK2 (IC50: 0.006 μM) inhibitor.

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CC-671 Chemical Structure
CC-671, CAS 1618658-88-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
5 mg In stock $ 113.00
10 mg In stock $ 189.00
25 mg In stock $ 378.00
50 mg In stock $ 568.00
100 mg In stock $ 815.00
500 mg In stock $ 1,680.00
1 mL * 10 mM (in DMSO) In stock $ 129.00
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Purity: 98.65%
Purity: 97.67%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CC-671 is a dual TTK protein kinase (IC50: 0.005 μM) /CLK2 (IC50: 0.006 μM) inhibitor.
Targets&IC50 CLK2:0.006 μM, TTK:0.005 μM
In vitro HCT-116 cell lysates treated with CC-671 at 3 μM for 1 h demonstrates that only four kinases show cellular binding of 75% or more including CLK2, CAMKK2, PIP4K22, and JNK[1].
In vivo CC-671 significantly inhibits tumor growth by 71% at doses of both 10 and 20 mg/kg on an every 3 days (q3d) dosing schedule, with no difference in efficacy between the two doses. However, it induces greater body weight loss at 20 mg/kg compared to 10 mg/kg (17% vs 5%)[1].
Kinase Assay The kinase selectivity profile of CC-671 is assessed. The screen is conducted with the concentration of CC-671 held constant at 3 μM. The TTK binding affinity is measured using the kinase binding assays. The kinase binding assays are based on the binding and displacement of a proprietary, Alexa Fluor 647-labeled, ATP-competitive kinase inhibitor scaffold[1].
Animal Research Female SCID mice are inoculated subcutaneously with 5×106 Cal-51 cells. Mice with tumours of approximately 125 mm3 are randomized and treated intravenously at various doses and schedules of CC-671 (n=8 to10/group). Tumours are measured twice a week for the duration of the study. The long and short axes of each a tumour are measured using a digital calliper in millimetres and the tumour volumes are calculated[1].
Molecular Weight 512.56
Formula C28H28N6O4
CAS No. 1618658-88-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (97.55 mM)

TargetMolReferences and Literature

1. Riggs JR, et al. The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatmentof Triple Negative Breast Cancer Initiated from a Phenotypic Screen. J Med Chem. 2017 Nov 9;60(21):8989-9002.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library NO PAINS Compound Library Cell Cycle Compound Library Preclinical Compound Library Anti-Cancer Compound Library Kinase Inhibitor Library

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Keywords

CC-671 1618658-88-0 Cell Cycle/Checkpoint Others CDK Inhibitor inhibit Cyclin dependent kinase CC 671 CC671 inhibitor

 

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