CC-671

SKU: orb1226044

Description

CC-671 is a potent, selective, dual TTK (Mps1)/CLK2 inhibitor with IC50 of 5/3 nM, respectively; weakly inhibits DYRK3, DYRK1A, PHKG, DYRK1B, and CLK1 with IC50 of 0.1-0.3 uM, and displays excellent kinase selectivity (7/235 kinases > 80% inhibition at 3 uM); inhibits autophosphorylation of TTK at T686 or phosphorylation of SR protein 75 with IC50 of 0.057 and 0.549 uM in Cal-51 cells; demonstrates strong single agent in vivo efficacy in multiple TNBC xenograft models without significant body weight loss.Breast Cancer Preclinical.

Key Properties

• CAS Number: 1618658-88-0
• MW: 512.57
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₈N₆O₄
• SMILES: O=C(NC)C1=CC=C(NC2=NC(OC3CCCC3)=C4C(NC=C4C5=CC=C6N=C(C)OC6=C5)=N2)C(OC)=C1
• Target: Mps1/TTK
• Solubility: DMSO: 60 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  CC-671 (compound 23) demonstrates significant tumor growth inhibition (TGI) ((vehicle-treated/vehicle) ×100%) of 71% at both 10 and 20 mg/kg on a every 3 days (q3d) dosing schedule. The body weight loss (BWL) in the CC-671 treated group (20 mg/kg) is higher than in the 10 mg/kg group (17% vs 5%).
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• In Vitro:
  CC-671 (compound 23) is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CC671 | CC 671

Quick Database Links

Gene Symbol

Mps1/TTK