A dual inhibitor of Mps1/TTK and Clk2
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CC-671

Item No. 26184

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[4-(cyclopentyloxy)-5-(2-methyl-6-benzoxazolyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxy-N-methyl-benzamide
CAS Number
1618658-88-0
Molecular Formula
C28H28N6O4
Formula Weight
512.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 10 mg/ml
λmax
282, 326 nm
SMILES
COC(C=C(C(NC)=O)C=C1)=C1NC2=NC(OC3CCCC3)=C(C(C4=CC=C(N=C(C)O5)C5=C4)=CN6)C6=N2
InChi Code
InChI=1S/C28H28N6O4/c1-15-31-21-10-8-16(12-23(21)37-15)19-14-30-25-24(19)27(38-18-6-4-5-7-18)34-28(33-25)32-20-11-9-17(26(35)29-2)13-22(20)36-3/h8-14,18H,4-7H2,1-3H3,(H,29,35)(H2,30,32,33,34)
InChi Key
CWJLAVRXVFHDSJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    Product Description

    CC-671 is a dual inhibitor of the spindle assembly checkpoint kinase Mps1/TTK and Cdc2-like kinase (Clk2; IC50s = 5 and 3 nM, respectively).1 It is selective for Mps1/TTK and Clk2 over a panel of 255 kinases at 3 μM, but does inhibit DYRK3, DYRK1A, PHKG, DYRK1B, and Clk1 (IC50s = 99, 104, 136, 157, and 300 nM, respectively). CC-671 selectively inhibits the growth of Cal-51 triple negative breast cancer (TNBC) cells over BT-474 luminal breast cancer cells (IC50s = 60 and 6,970 nM, respectively). In vivo, CC-671 (20 mg/kg) reduces tumor volume in a Cal-51 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Riggs, J.R., Nagy, M., Elsner, J., et al. The discovery of a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor for the treatment of triple negative breast cancer initiated from a phenotypic screen. J. Med. Chem. 60(21), 8989-9002 (2017).