Zidesamtinib

CAS No. 2739829-00-4

Zidesamtinib( —— )

Catalog No. M36481 CAS No. 2739829-00-4

Zidesamtinib (NVL-520) is an orally active, selective, potent, and blood-brain-barrier-crossing inhibitor of ROS1 fusion and resistance mutations, inhibits ROS1 and ROS1 G2032R, and can be used in the study of non-small-cell lung cancer and solid tumors.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 248 Get Quote
5MG 353 Get Quote
10MG 629 Get Quote
25MG 1067 Get Quote
50MG 1444 Get Quote
100MG 2007 Get Quote
200MG 2664 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Zidesamtinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Zidesamtinib (NVL-520) is an orally active, selective, potent, and blood-brain-barrier-crossing inhibitor of ROS1 fusion and resistance mutations, inhibits ROS1 and ROS1 G2032R, and can be used in the study of non-small-cell lung cancer and solid tumors.
  • Description
    Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.
  • In Vitro
    Zidesamtinib (72 h) inhibits the growth of seven cell lines expressing wild-type ROS1 fusions, with average IC50s of 0.4 nM.Zidesamtinib (72 h) inhibits the growth of six cell lines harboring ROS1 fusions with the G2032R mutation, with average IC50s of 1.6 nM.Zidesamtinib (72 h) potently inhibits the non-G2032R ROS1 mutants, with IC50s ≤ 1.5 nM.Zidesamtinib (10-1000 nM; 4 weeks) suppresses colony formation in NIH3T3 cells expressing wild-type ROS1 fusions and expressing ROS1 fusions with G2032R.
  • In Vivo
    Zidesamtinib (0.04-15 mg/kg; p.o. twice daily for 28 d) induces tumor regression at all doses ≥0.2 mg/kg in wild-type ROS1 xenograft models.Animal Model:Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848.Dosage:0.04, 0.2, 1, 5, 15 mg/kg Administration:Oral gavage twice daily for 21 days Result:Inhibited the tumor volumes.
  • Synonyms
    ——
  • Pathway
    Immunology/Inflammation
  • Target
    ROS
  • Recptor
    ROS Kinase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2739829-00-4
  • Formula Weight
    419.455
  • Molecular Formula
    C22H22FN7O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (119.20 mM; Ultrasonic ( 65°C)
  • SMILES
    C(C)N1C2=C(CC=3C(C=4C([C@@H](C)OC=5C=C2C=NC5N)=CC(F)=CC4)=NN(C)N3)C=N1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Drilon A, et, al. NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations. Cancer Discov. 2022 Dec 13;CD-22-0968.?
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