A RET inhibitor
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TPX-0046

Item No. 41990

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3aS,11R,20aR)-7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-17,19-metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one
CAS Number
2359650-19-2
Synonyms
  • Enbezotinib
Molecular Formula
C21H21FN6O3
Formula Weight
424.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=C2N=C3C(O[C@@](CCC4)([H])[C@@]4([H])N3CC(C=C(F)C=N5)=C5O6)=CN2N=C1)NC[C@H]6C
InChi Code
InChI=1S/C21H21FN6O3/c1-11-6-23-20(29)14-8-25-28-10-17-19(26-18(14)28)27(15-3-2-4-16(15)31-17)9-12-5-13(22)7-24-21(12)30-11/h5,7-8,10-11,15-16H,2-4,6,9H2,1H3,(H,23,29)/t11-,15+,16-/m1/s1
InChi Key
BYYQDEOVMILBQT-XFBWCDHKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $99

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    5 mg

    $446

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    10 mg

    $792

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    25 mg

    $1,733

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    Product Description

    TPX-0046 is a RET inhibitor (IC50 = 0.26 nM for the wild-type enzyme).1 It is selective for RET over a panel of 217 additional kinases but does inhibit 39 tyrosine kinases by greater than 50% at 26 nM. TPX-0046 inhibits the phosphorylation of wild-type RET (IC50 = 21.9 nM) and 15 RET mutants (IC50s = 2.69-108 nM) in Ba/F3 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miyazaki, I., Odintsov, I., Ishida, K., et al. Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations. Nat. Cancer 4(9), 1345-1361 (2023).