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LP-184

编号: 24121
Cas号: 924835-67-6
纯度: 98% Min.

 LP-184 is an acylfulvene-derived prodrug activated by the oxidoreductase PTGR1 that alkylates at N3-adenine. Cytotoxicity of LP-184 is solely dependent on prostaglandin reductase 1 (PTGR1). LP-184 metabolizes to an active compound by the oxidoreductase activity of enzyme prostaglandin reductase 1 (PTGR1), which is frequently elevated in multiple solid tumor types.


仅供研究使用。 我们不向患者出售。

化学信息

名称LP-184
Iupac 化学名称 (R)-1-hydroxy-1-((6'-hydroxy-2',4',6'-trimethyl-7'-oxo-6',7'-dihydrospiro[cyclopropane-1,5'-inden]-3'-yl)methyl)urea
同义词LP-184; LP184; LP 184;
英文同义词LP-184; LP184; LP 184;
分子式C16H20N2O4
分子量304.34
SmileCC1=C(CN(O)C(N)=O)C2=C(C)C3(CC3)[C@@](C)(O)C(=O)C2=C1
InChiKeyVWMPVAZEBAKLFR-HNNXBMFYSA-N
InChiInChI=1S/C16H20N2O4/c1-8-6-10-12(11(8)7-18(22)14(17)20)9(2)16(4-5-16)15(3,21)13(10)19/h6,21-22H,4-5,7H2,1-3H3,(H2,17,20)/t15-/m0/s1
Cas号924835-67-6
相关CAS号

订购信息

包装价格库存纯度备货期
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外观性状Off-white solid
纯度98% Min.
存储Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
可溶性Soluble in DMSO
处理方式
运输条件Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Lal B, Kulkarni A, McDermott J, Rais R, Alt J, Wu Y, Lopez-Bertoni H, Sall S, Kathad U, Zhou J, Slusher BS, Bhatia K, Laterra J. Preclinical Efficacy of LP-184, a Tumor Site Activated Synthetic Lethal Therapeutic, in Glioblastoma. Clin Cancer Res. 2023 Oct 13;29(20):4209-4218. doi: 10.1158/1078-0432.CCR-23-0673. PMID: 37494541.


2: Restifo D, McDermott JR, Cvetkovic D, Dos Santos T, Ogier C, Surumbayeva A, Handorf EA, Schimke C, Ma C, Cai KQ, Olszanski AJ, Kathad U, Bhatia K, Sharma P, Kulkarni A, Astsaturov I. Conditional Dependency of LP-184 on Prostaglandin Reductase 1 is Synthetic Lethal in Pancreatic Cancers with DNA Damage Repair Deficiencies. Mol Cancer Ther. 2023 Oct 2;22(10):1182-1190. doi: 10.1158/1535-7163.MCT-22-0818. PMID: 37552607; PMCID: PMC10592171.


3: Kulkarni A, Zhou J, Biyani N, Kathad U, Banerjee PP, Srivastava S, Prucsi Z, Solarczyk K, Bhatia K, Ewesuedo RB, Sharma P. LP-184, a Novel Acylfulvene Molecule, Exhibits Anticancer Activity against Diverse Solid Tumors with Homologous Recombination Deficiency. Cancer Res Commun. 2024 May 6;4(5):1199-1210. doi: 10.1158/2767-9764.CRC-23-0554. PMID: 38630886; PMCID: PMC11072798.


4: Kulkarni A, McDermott JR, Kathad U, Modali R, Richard JP, Sharma P, Bhatia K. The acylfulvene alkylating agent, LP-184, retains nanomolar potency in non-small cell lung cancer carrying otherwise therapy-refractory mutations. Oncotarget. 2021 Apr 13;12(8):791-806. doi: 10.18632/oncotarget.27943. PMID: 33889302; PMCID: PMC8057270.


5: Kathad U, Kulkarni A, McDermott JR, Wegner J, Carr P, Biyani N, Modali R, Richard JP, Sharma P, Bhatia K. A machine learning-based gene signature of response to the novel alkylating agent LP-184 distinguishes its potential tumor indications. BMC Bioinformatics. 2021 Mar 2;22(1):102. doi: 10.1186/s12859-021-04040-8. PMID: 33653269; PMCID: PMC7923321.


6: Staake MD, Kashinatham A, McMorris TC, Estes LA, Kelner MJ. Hydroxyurea derivatives of irofulven with improved antitumor efficacy. Bioorg Med Chem Lett. 2016 Apr 1;26(7):1836-8. doi: 10.1016/j.bmcl.2016.02.028. Epub 2016 Feb 13. PMID: 26922141.


7: Sung ES, Kim JH. The difference effect of estrogen on muscle tone of medial and lateral thigh muscle during ovulation. J Exerc Rehabil. 2018 Jun 30;14(3):419-423. doi: 10.12965/jer.1836110.055. PMID: 30018928; PMCID: PMC6028216.

化学结构

24121 - LP-184 | CAS 924835-67-6

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