1. Protein Tyrosine Kinase/RTK
  2. ALK
    ROS
    Trk Receptor

TPX-0005 

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

TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.

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

TPX-0005 Chemical Structure

TPX-0005 Chemical Structure

CAS No. : 1802220-02-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 590 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.

IC50 & Target

IC50: 5.3 nM (SRC), 1.01 nM (WT ALK), 1.26 nM (ALK G1202R), 1.08 nM (ALK L1196M)[1]

In Vitro

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). PX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib[1].

In Vivo

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

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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.
References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 83.3 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.91%

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Product Name:
TPX-0005
Cat. No.:
HY-103022
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