1. Protein Tyrosine Kinase/RTK
    Neuronal Signaling
  2. ROS
    Trk Receptor
    ALK
  3. Repotrectinib

Repotrectinib (Synonyms: TPX-0005)

Cat. No.: HY-103022 Purity: 99.91%
Handling Instructions

Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. Repotrectinib (TPX-0005) potently inhibits WT ALK (1.01 nM) and mutant ALKs including ALK G1202R (1.26 nM) and ALK L1196M (1.08 nM). It also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (1.04, 1.66, 5.3, and 6.96 nM, respectively) .

For research use only. We do not sell to patients.

Repotrectinib Chemical Structure

Repotrectinib Chemical Structure

CAS No. : 1802220-02-5

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Based on 1 publication(s) in Google Scholar

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Description

Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. Repotrectinib (TPX-0005) potently inhibits WT ALK (1.01 nM) and mutant ALKs including ALK G1202R (1.26 nM) and ALK L1196M (1.08 nM). It also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (1.04, 1.66, 5.3, and 6.96 nM, respectively) [1][2].

IC50 & Target

IC50: 0.07 nM (ROS1), 0.83/0.05/0.1 nM (TRKA/B/C), 1.01 nM (ALK), 1.04 nM (JAK2), 1.66 nM (LYN), 5.3 nM (Src), 6.96 nM (FAK)[1][2]

In Vitro

Repotrectinib (TPX-0005) effectively overcomes this primary resistance (IC50 100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50 13 nM) and the SRC substrate paxillin (IC50 107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib[1].

In Vivo

Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[1].

Clinical Trial
Molecular Weight

355.37

Formula

C₁₈H₁₈FN₅O₂

CAS No.

1802220-02-5

SMILES

O=C1NC[[email protected]](C)OC2=CC=C(F)C=C2[[email protected]@H](C)NC3=NC4=C1C=NN4C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (234.40 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8140 mL 14.0698 mL 28.1397 mL
5 mM 0.5628 mL 2.8140 mL 5.6279 mL
10 mM 0.2814 mL 1.4070 mL 2.8140 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.91%

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Keywords:

RepotrectinibTPX-0005TPX0005TPX 0005ROSTrk ReceptorALKTropomyosin related kinase receptor Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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Repotrectinib
Cat. No.:
HY-103022
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