SP2509
分子式：C₁₉H₂₀ClN₃O₅S分子量：437.90
简介 ：SP2509 是有效，选择性的LSD1拮抗剂，IC50值为 13 nM。
物理性状及指标：
外观：……………………粉末
溶解性：…………………DMSO : ≥ 33 mg/mL(75.36 mM)；H2O : < 0.1 mg/mL(insoluble)
含量：……………………>98%,BR
储存条件：-20°C，避光防潮密闭干燥
运输条件：常温运输
生物活性
|
描述
|
SP2509 is a potent and selective antagonist oflysine specific demethylase 1 (LSD1)withIC50of 13 nM. |
|
IC50& Target |
IC50: 13 nM (LSD1) |
|
体外 |
SP2509 (250, 500, 1000 nM) inhibits LSD1 activity, depletes colony growth and induces apoptosis and cell death of cultured human acute myeloid leukemia cells, and increases H3K4Me3 on the promoters of p57 Kip, KLF4, and p21 and induces mRNA expression of p57Kip, KLF4 and p21 in AML cells. SP2509 (250, 1000 nM) induces features of morphologic differentiation of cultured and primary AML cells. Besides, SP2509 in combination with PS exerts synergistic lethal activity against cultured and primary AML cells. SP2509 does not destabilize the CoREST-LSD1 interaction, and has no major destabilizing effect on the CRC. SP2509 (1 or 10 µM) induces cell death, but there are no morphological changes at a low concertation of 0.1 µM. SP2509 likewise interferes with the viability of medulloblastoma cells. |
|
体内 |
Treatment with SP2509 (25 mg/kg) and/or PS (5 mg/kg) significantly enhances PS-mediated loss of viability of CD34+primary AML cells and improves the survival of mice bearing AML xenografts and primagrafts. |
实验参考方法（仅来自公开文献，供参考）
| 细胞实验： | Daoy and D283 Med cells are used in the assay. ONS-76 cells used. All medulloblastoma cell lines are kept in an incubator at 37°C in a 5% CO2/5% O2/90% N2atmosphere with maximum humidity. XTT assays are performed in triplicates (n = 3) with three replicates for each using 1×103Daoy cells/well, 4×103D283 Med cells/well, and 1×103ONS-76 cells/well in 100 µL of medium at initial seeding in 96-well plates. |
|
动物实验 |
Female NOD/SCID mice are exposed to 2.5 Gy of radiation. The following day, 5 million OCI-AmL3 cells are injected into the lateral tail vein of the mice and the mice are monitored for 7 days. Following treatments are administered in cohorts of 8 mice for each treatment: vehicle alone, 25 mg/kg SP2509, 5 mg/kg LBH589 and SP2509 plus LBH589. Treatments are initiated on day 7 for OCI-AmL3 cells. SP2509 (formulated in solubilization buffer [20% Cremaphor, 20% DMSO, 60% sterile water]) is administered twice per week (Tues and Thurs) intraperitoneally (IP) for 3 weeks, and then discontinued. LBH589 (formulated in 5% DMSO/ 95% normal saline) is administered by IP injection 3 days per week (M-W-F) for 3 weeks and discontinued. The doses of PS utilized in these studies are determined to be safe and effective. A separate in vivo experiment is conducted utilizing NSG mice and primary AmL cells. Following engraftment of the AmL cells (presence of greater than 1% CD45+cells in the peripheral blood), mice are treated with SP2509 and/or PS, for three weeks. |
美仑相关产品推荐(更多相关靶点抑制剂请详询官网或客服)
|
MB1666
|
Sorafenib |
|
MB6045 |
LY294002 |
|
MB5603 |
JIB-04 |
储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
 |
1 mg |
5 mg |
10 mg |
|
1 mM |
2.2836 mL |
11.4181 mL |
22.8363 mL |
|
5 mM |
0.4567 mL |
2.2836 mL |
4.5673 mL |
|
10 mM |
0.2284 mL |
1.1418 mL |
2.2836 mL |
【注意 】
●我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。
●部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，以上数据仅供参考交流研究之用。
我司所售出产品仅供于科研研究用途（非临床科研研究），每次销售产品行为都适用于我司网上所列明的通用销售条款。