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首页-小分子抑制剂&激动剂-Tyrosine Kinase-ROS1-NVL-520
NVL-520

Chemical Structure : NVL-520

CAS No.: 2739829-00-4

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NVL-520 (Zidesamtinib, NVL520)

货号: PC-49635Not For Human Use, Lab Use Only.

Zidesamtinib (NVL-520, NVL520) is a potent, selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations with IC50 of 0.5-3.5 nM, and 12 nM for ROS1 WT.

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5 mg ￥3580 In stock
10 mg ￥5280 In stock
25 mg ￥7980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Zidesamtinib (NVL-520, NVL520) is a potent, selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations with IC50 of 0.5-3.5 nM, and 12 nM for ROS1 WT.
Zidesamtinib (NVL-520) displays >50-fold ROS1 selectivity over 98% of the kinome tested.
Zidesamtinib (NVL-520) is active in vitro against diverse ROS1 fusions and resistance mutations and exhibits 10-to-1,000-fold improved potency for the ROS1 G2032R solvent-front mutation over crizotinib, entrectinib, lorlatinib, taletrectinib, and repotrectinib.
Zidesamtinib (NVL-520) induces tumor regression in G2032R-inclusive intracranial and patient-derived xenograft models.
NVL-520 has a ~100-fold increased potency for ROS1 and ROS1 G2032R over TRK.
In clinical investigations, NVL-520 elicited objective tumor responses in three patients with TKI-refractory ROS1 fusion-positive lung cancers, including two with ROS1 G2032R and one with intracranial metastases, with no observed neurological toxicities.

物理化学性质&存储条件

分子量 419.46
分子式 C22H22FN7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(14R)-7-Ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-7H-8,12-metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine

参考文献

1. Alexander Drilon, et al. Cancer Discov. 2022 Dec 13;CD-22-0968.

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