A dual inhibitor of FAK1 and ALK
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CEP-37440

Item No. 21278

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[5-chloro-2-[[(6S)-6,7,8,9-tetrahydro-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-N-methyl-benzamide
CAS Number
1391712-60-9
Molecular Formula
C30H38ClN7O3
Formula Weight
580.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
279, 333 nm
SMILES
O=C(NC)C1=CC=CC=C1NC2=NC(NC3=C(OC)C(CCC[C@H](N4CCN(CCO)CC4)C5)=C5C=C3)=NC=C2Cl
InChi Code
InChI=1S/C30H38ClN7O3/c1-32-29(40)23-7-3-4-9-25(23)34-28-24(31)19-33-30(36-28)35-26-11-10-20-18-21(6-5-8-22(20)27(26)41-2)38-14-12-37(13-15-38)16-17-39/h3-4,7,9-11,19,21,39H,5-6,8,12-18H2,1-2H3,(H,32,40)(H2,33,34,35,36)/t21-/m0/s1
InChi Key
BCSHRERPHLTPEE-NRFANRHFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CEP-37440 is a dual inhibitor of focal adhesion kinase 1 (FAK1; IC50s = 2.0 and 80 nM for in vitro enzyme and cellular inhibition, respectively) and anaplastic lymphoma kinase (ALK; IC50s = 3.1 and 22 nM for in vitro enzyme and cellular inhibition, respectively).1,2 It blocks the proliferation of inflammatory and triple-negative breast cancer cell lines but not normal breast epithelial cells.2 CEP-37440 reduces the growth and metastasis of breast cancer xenografts in mice when given by oral gavage.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ott, G.R., Cheng, M., Learn, K.S., et al. Discovery of clinical candidate CEP-37440, a selective inhibitor of focal adhesion kinase (FAK) and anaplastic lymphoma kinase (ALK). J. Med. Chem. 59(16), 7478-7496 (2016).

    2. Salem, I., Alsalahi, M., Chervoneva, I., et al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 18(1), 37 (2016).