LP-184 (Zirdafulven, LP184)

Chemical Structure : LP-184

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货号: PC-22197Not For Human Use, Lab Use Only.

LP-184 (Zirdafulven, LP184) is an acylfulvene alkylating agent, inhibits viability of multiple GBM cell isolates including temozolomide-resistant and MGMT-expressing cells with IC50 of 22-310 nM.

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生物&药学活性

LP-184 (Zirdafulven, LP184) is an acylfulvene alkylating agent, inhibits viability of multiple GBM cell isolates including temozolomide-resistant and MGMT-expressing cells with IC50 of 22-310 nM.
LP-184 demonstrated highly potent anticancer activity both in primary NSCLC cell lines and in those originating from brain metastases of primary lung cancers.
LP-184 activity correlated with PTGR1 transcript levels but was independent of mutations in key oncogenes (KRAS and KEAP1) and tumor suppressors (TP53 and STK11).
LP-184 was orders of magnitude more potent in vitro than cisplatin and pemetrexed.
LP-184 is an acylfulvene-derived prodrug activated by the oxidoreductase PTGR1 that alkylates at N3-adenine.

物理化学性质&存储条件

分子量	304.35
分子式	C16H20N2O4
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-hydroxy-1-((6'-hydroxy-2',4',6'-trimethyl-7'-oxo-6',7'-dihydrospiro[cyclopropane-1,5'-inden]-3'-yl)methyl)urea

参考文献

1. Kulkarni A, et al. Cancer Res Commun. 2024 Apr 17. doi: 10.1158/2767-9764.CRC-23-0554.

2. Lal B, et al. Clin Cancer Res. 2023 Oct 13;29(20):4209-4218.

3. Kulkarni A, et al. Oncotarget. 2021 Apr 13;12(8):791-806.