A multi-kinase inhibitor
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TPX-0005

Item No. 23397

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(7S,13R)-11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one
CAS Number
1802220-02-5
Synonyms
  • Repotrectinib
Molecular Formula
C18H18FN5O2
Formula Weight
355.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 0.2 mg/mlDMSO: Slightly soluble: 0.1-1 mg/mL
λmax
222, 258 nm
SMILES
C[C@@H](NC1=NC2=C3C=NN2C=C1)C4=CC(F)=CC=C4O[C@@H](C)CNC3=O
InChi Code
InChI=1S/C18H18FN5O2/c1-10-8-20-18(25)14-9-21-24-6-5-16(23-17(14)24)22-11(2)13-7-12(19)3-4-15(13)26-10/h3-7,9-11H,8H2,1-2H3,(H,20,25)(H,22,23)/t10-,11+/m0/s1
InChi Key
FIKPXCOQUIZNHB-WDEREUQCSA-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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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    TPX-0005 is a multi-kinase inhibitor that inhibits TrkA, TrkB, and TrkC (IC50s = 0.83, 0.05, and 0.1 nM, respectively) as well as C-ros oncogene 1 (ROS1; IC50 = 0.07 nM).1 It inhibits a variety of other kinases, including ALK, JAK2, LYN, Src, and FAK (IC50s = 1.04, 1.04, 1.66, 5.3, and 6.96 nM, respectively). It inhibits proliferation of PC-9, H1975, 11-18, HCC4006, and HCC827 lung cancer cells (IC50s = 100, 100, 150, 148, and 430 nM, respectively) with additive or synergistic effects when used in combination with gefitinib (Item No. 13166), afatinib (Item No. 11492), PF-299804 (dacomitinib; Item No. 9001879), or osimertinib. TPX-0005 (30 mg/kg) reduces tumor growth in PC-9 and H1975 mouse xenograft models and potentiates the effect of osimertinib in these models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Karachaliou, N., Chaib, I., Cardona, A.F., et al. Common co-activation of AXL and CDCP1 in EGFR-mutation-positive non-smallcell lung cancer associated with poor prognosis. EBioMedicine 29, 112-127 (2018).