Neladalkib (NVL-655) | ALK inhibitor | Probechem Biochemicals

Chemical Structure : NVL-655

CAS No.: 2739866-40-9

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NVL-655 (Neladalkib, NVL655)

货号: PC-23342Not For Human Use, Lab Use Only.

Neladalkib (NVL-655) is a potent, selective and brain-penetrant fourth-generation inhibitor of diverse ALK-mutant oncoproteins with IC50 of 0.9 nM and 1.8 nM for WT ALK and ALK G1202R/L1196M mutant respectively.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥2180	In stock
50 mg	￥3480	In stock
100 mg	￥5480	In stock
250 mg		Get quote

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生物&药学活性

Neladalkib (NVL-655) is a potent, selective and brain-penetrant fourth-generation inhibitor of diverse ALK-mutant oncoproteins with IC50 of 0.9 nM and 1.8 nM for WT ALK and ALK G1202R/L1196M mutant respectively.
Neladalkib (NVL-655) potently inhibits cell lines expressing WT ALK fusions with average IC50 < 1.1 nM.
Neladalkib (NVL-655) exhibits an IC50 of 0.3 to 1.6 nM against MGH048-1, MGH064-1, and MGH026-1 cell lines, which were established from TKI-naïve patients with NSCLC harboring EML4–ALK v1, v2, and v3 fusions, respectively, and IC50 of 2 nM against the anaplastic large cell lymphoma cell line Karpas299 harboring the NPM1–ALK fusion.
Neladalkib (NVL-655) potently inhibits the growth of cell lines harboring ALKG1202R fusions (IC50 = 0.1–0.8 nmol/L, average
< 0.3 nM), including three PDCs established after progressive disease on alectinib (MGH953-4 and YU1077) or brigatinib (MGH9037-2).
Neladalkib (NVL-655) is >14-fold more potent than zotizalkib, >100 fold more potent than lorlatinib, and >280-fold more potent
than 1G and 2G ALK TKIs on average.
Neladalkib (NVL-655) inhibits ALK over TRK with 22-fold to >874-fold selectivity.
Neladalkib (NVL-655) demonstrates preliminary proof-of-concept clinical activity in heavily pretreated patients with ALK fusion-positive non-small cell lung cancer, including in patients with brain metastases and single or compound ALK resistance mutations.

物理化学性质&存储条件

分子量	452.92
分子式	C23H22ClFN6O
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	(R)-1-Chloro-3-ethyl-12-fluoro-10,16-dimethyl-3,10,16,18-tetrahydro-4,8-(metheno)benzo[l]dipyrazolo[3,4-g:4',3'-j][1]oxa[4]azacyclotetradecin-7-amine

参考文献

1. Lin JJ, et al. Cancer Discov. 2024 Sep 13:OF1-OF20.

NVL-655 (Neladalkib, NVL655)

生物&药学活性

物理化学性质&存储条件

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NVL-655 (Neladalkib, NVL655)

生物&药学活性

物理化学性质&存储条件

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