| Identification | Back Directory | [Name]
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- | [CAS]
2739829-00-4 | [Synonyms]
NVL-520
Zidesamtinib
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- | [Molecular Formula]
C22H22FN7O | [MOL File]
2739829-00-4.mol | [Molecular Weight]
419.46 |
| Chemical Properties | Back Directory | [Boiling point ]
685.7±65.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
7.43±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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[1].
| Animal Model: | Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848[1] | | Dosage: | 0.04, 0.2, 1, 5, 15 mg/kg
| | Administration: | Oral gavage twice daily for 21 days
| | Result: | Inhibited the tumor volumes. |
| [References]
[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. DOI:10.1158/2159-8290.CD-22-0968 |
| Spectrum Detail | Back Directory | [Spectrum Detail]
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)-(2739829-00-4)1HNMR
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