An inhibitor of RETM918T and a derivative of sorafenib
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APS6-45

Item No. 38417

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide
CAS Number
2188236-41-9
Molecular Formula
C23H16F8N4O3
Formula Weight
548.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
260 nm
SMILES
O=C(NC1=CC(C(C(F)(F)F)(C(F)(F)F)F)=CC=C1F)NC2=CC=C(C=C2)OC3=CC=NC(C(NC)=O)=C3
InChi Code
InChI=1S/C23H16F8N4O3/c1-32-19(36)18-11-15(8-9-33-18)38-14-5-3-13(4-6-14)34-20(37)35-17-10-12(2-7-16(17)24)21(25,22(26,27)28)23(29,30)31/h2-11H,1H3,(H,32,36)(H2,34,35,37)
InChi Key
MVUPJRHPAMCBQJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    APS6-45 is an inhibitor of RETM918T and a derivative of sorafenib (Item No. 10009644 | 35612).1 It selectively binds to RETM918T over Eph tyrosine kinase receptor A8 (EphA8), p38δ, JNK2, and c-Src (Kds = 28, 410, 940, 1,500, and 1,700 nM, respectively), as well as a panel of over 60 kinases at 10 µM, but also binds to cyclin-dependent kinase 14 (Cdk14), MAP4K4, and protein tyrosine kinase 5 (PTK5; Kds = 55, 130, and 140 nM, respectively). It inhibits TT medullary thyroid carcinoma cell colony formation when used at a concentration of 30 nM. APS6-45 (10 mg/kg per day) decreases tumor volume in a TT mouse xenograft model. It increases survival to adulthood in Drosophila expressing the lethal RetM955T mutation in a concentration-dependent manner. APS6-45 (100 µM) prevents the development of a rough-eye phenotype induced by RetM955T in Drosophila.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shonoshita, M., Scopton, A.P., Ung, P.M.U., et al. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat. Chem. Biol. 14(3), 291-298 (2018).