An inhibitor of ULK1/2
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DCC-3116

Item No. 45313

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[3-[[2-[[2-ethyl-4-(4-methyl-1-piperazinyl)phenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]propyl]tetrahydro-1,4-oxazepin-5(2H)-one
CAS Number
2543673-19-2
Synonyms
  • Inlexisertib
Molecular Formula
C26H36F3N7O2
Formula Weight
535.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CN1CCN(C2=CC=C(NC(N=C3NCCCN4CCOCCC4=O)=NC=C3C(F)(F)F)C(CC)=C2)CC1
InChi Code
InChI=1S/C26H36F3N7O2/c1-3-19-17-20(35-12-10-34(2)11-13-35)5-6-22(19)32-25-31-18-21(26(27,28)29)24(33-25)30-8-4-9-36-14-16-38-15-7-23(36)37/h5-6,17-18H,3-4,7-16H2,1-2H3,(H2,30,31,32,33)
InChi Key
CNBTYICEJGEABG-UHFFFAOYSA-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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    10 mg

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    Product Description

    DCC-3116 is an inhibitor of unc-51-like autophagy activating kinase 1/2 (ULK1/2).1 It decreases phosphorylation of the ULK1 substrate ATG13 in NCI H2122, Calu-1, and NCI H358 non-small cell lung cancer (NSCLC) cells, which express the activating K-RasG12C mutation, at 2 µM. It also reduces basal autophagy and autophagy induced by the K-RasG12C inhibitor sotorasib (AMG 510; Item No. 29465) in the same cells. DCC-3116 (2 µM) inhibits the proliferation of Calu-1 and NCI H358 cells, with a synergistic effect when used in combination with sotorasib in NCI H2122 and Calu-1, but not NCI H358, cells. It cooperatively increases sotorasib-induced reductions in tumor volume in NCI H2122 and Calu-1 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ghazi, P.C., O'Toole, K.T., Srinivas Boggaram, S., et al. Inhibition of ULK1/2 and KRASG12C controls tumor growth in preclinical models of lung cancer. Elife. 13, RP96992 (2024).