TPX-0005 free base · Synonyms: Repotrectinib

Repotrectinib is a potent ROS1 and TRK inhibitor.

For research use only. Not for human or veterinary use.

Target ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK)

Research area Cancer

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Data Sheet SDS COA

TPX-0005 structure

CAS No.: 1802220-02-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 g	USD 580.00	BP-01929-5g	In stock	Get quote
10 g	USD 1,050.00	BP-01929-10g	In stock	Get quote
25 g	Inquire	BP-01929-25g	In stock	Inquire

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Description

Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.

Biological activity

In Vitro Repotrectinib (TPX-0005) inhibits mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM). Repotrectinib also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (IC50=1.04, 1.66, 5.3, and 6.96 nM, respectively). Repotrectinib 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. In Vivo Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts.

Identifiers

SMILES: C[C@H]1CNC(=O)C2=C3N=C(N[C@H](C)C4=CC(F)=CC=C4O1)C=CN3N=C2
InChIKey: FIKPXCOQUIZNHB-WDEREUQCSA-N

Specifications

MW (average): 355.3662
Formula: C₁₈H₁₈FN₅O₂
CAS No.: 1802220-02-5
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016

[2]. Karachaliou N, et al. Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis. EBioMedicine. 2018 Mar;29:112-127.

Same target

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Same research area

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