| Identification | Back Directory | [Name]
6-methyl-2-[2-[(E)-(6-oxo-1-cyclohexa-2,4-dienylidene)methyl]hydraziny l]-1H-pyrimidin-4-one | [CAS]
66680-03-3 | [Synonyms]
NSC 73150
XVDNTAIBZHGIAL-UHFFFAOYSA-N
Benzaldehyde, 2-hydroxy-, 2-(1,6-dihydro-4-methyl-6-oxo-2-pyrimidinyl)hydrazone
6-methyl-2-[2-[(E)-(6-oxo-1-cyclohexa-2,4-dienylidene)methyl]hydraziny l]-1H-pyrimidin-4-one
6 methyl 2 [2 [(E) (6 oxo 1 cyclohexa 2,4 dienylidene)methyl]hydraziny l] 1H pyrimidin 4 one,6methyl2[2[(E)(6oxo1cyclohexa2,4dienylidene)methyl]hydraziny l]1Hpyrimidin4one | [Molecular Formula]
C12H12N4O2 | [MDL Number]
MFCD00023205 | [MOL File]
66680-03-3.mol | [Molecular Weight]
244.25 |
| Hazard Information | Back Directory | [Uses]
SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis[1]. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) [2]. | [in vivo]
SKLB325 (10 mg/kg) has antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, and A2780s tumor growth in nude mice[1]. | Animal Model: | Female athymic BALB/c nude mice[1] | | Dosage: | 10?mg/kg | | Administration: | I.p. injections every three days for eight doses total | | Result: | The average weight of intraperitoneal tumor nodules was 1.56?±?0.70, 1.04?±?0.62, and 0.14?±?0.11?g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.
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| [References]
[1] Heng Zheng, et al. Jumonji domain-containing 6 (JMJD6) identified as a potential therapeutic target in ovarian cancer. Signal Transduct Target Ther.2019 Jul 26;4:24. DOI:10.1038/s41392-019-0055-8
[2] Chuanjie Zhang, et al. Epigenome screening highlights that JMJD6 confers an epigenetic vulnerability and mediates sunitinib sensitivity in renal cell carcinoma. Clin Transl Med. 2021 Feb;11(2):e328. DOI:10.1002/ctm2.328 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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