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Repotrectinib

SKU T4071-1 mL * 10 mM (in DMSO) Category Small Compound Brand: TargetMol

Price range: 72 CAD through 1,160 CAD

For Research Use Only (RUO). This product is sold strictly for laboratory research use. Not for human or veterinary consumption, therapeutic, or diagnostic use.For sale to research organizations and laboratories only; not for patients or for personal use.

Size

2 mg 1 mg 1 mL * 10 mM (in DMSO)10 mg 100 mg 25 mg 5 mg 50 mg

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Products Details

Product Description

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

For Research Use Only (RUO). This product is sold strictly for laboratory research use only. Not for human or veterinary consumption, therapeutic, or diagnostic use. Any pharmacological, therapeutic, cosmetic, or biological effects described above are provided as research context only and do not represent intended or approved uses of this product.

Web ID

– T4071

Storage Temperature

– -20℃

Shipping

– Blue Ice

Molecular Formula

– C18H18FN5O2

Citations

– 1. Li W, Sparidans R W, Lebre M C, et al. ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, while OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability[J. Pharmaceutics. 2021, 13(11): 1761 2. Li W, Perpinioti N, Schinkel A H, et al. Bioanalytical assay for the new-generation ROS1/TRK/ALK inhibitor repotrectinib in mouse plasma and tissue homogenate using liquid chromatography-tandem mass spectrometry. Journal of Chromatography B. 2020: 122098 3. Jin X, Liu D, Zhou X, et al.Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7.Cell Reports Medicine.2023, 4(12). 4. Li W, Sparidans R W, Wang Y, et al.Interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and ABCG2 efflux transporters in the handling of bilirubin and drugs.Biomedicine & Pharmacotherapy.2024, 175: 116644. 5. Cen S Y, Lin F, Li X, et al.Crizotinib and its enantiomer suppress ferroptosis by decreasing PE-O-PUFA content.Cell Death Discovery.2024, 10(1): 360.

References

– 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

CAS Number

– 1802220-02-5

Molecular Weight

– C18H18FN5O2

Compound Purity

– 0.9992

SMILES

– C[C@H]1CNC(=O)c2cnn3ccc(N[C@H](C)c4cc(F)ccc4O1)nc23

Pathway

– Angiogenesis|||Tyrosine Kinase/Adaptors|||Immunology/Inflammation

Product type

– Small Compound

Booklet

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.