SP2509

別名: HCI-2509

目錄號(hào)：S7680 Purity: 99.99%

SP2509 (HCI-2509)是一種選擇性histone demethylase LSD1抑制劑，IC50為 13?nM，對MAO-A，MAO-B，乳酸脫氫酶和葡萄糖氧化酶沒有活性。SP2509 可誘導(dǎo)凋亡并促進(jìn)自噬。

SP2509 Chemical Structure

CAS: 1423715-09-6

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1367.73	現(xiàn)貨
5mg	1204.84	現(xiàn)貨
25mg	3883.86	現(xiàn)貨
100mg	8155.08	現(xiàn)貨
1g	12039.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

SP2509相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	KDM1 KDM2 KDM3 KDM4 KDM5 KDM6	點(diǎn)擊展開
相關(guān)產(chǎn)品	GSK J4 HCl CPI-455 HCl Iadademstat (ORY-1001) 2HCl GSK-LSD1 2HCl JIB-04 OG-L002 ML324 IOX1 GSK J1 CP2 CPI-455	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 FDA藥物庫天然產(chǎn)物庫已知活性藥物庫-I 高選擇性抑制劑庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息(PMID)
HT-29	Growth inhibition assay	96 h	Growth inhibition of human HT-29 cells after 96 hrs by ATPlite luminescence assay IC50=0.429 μM	24237195
MCF7	Growth inhibition assay	96 h	Growth inhibition of human MCF7 cells after 96 hrs by ATPlite luminescence assay IC50=0.637 μM	24237195
MDA-MB-231	Growth inhibition assay	96 h	Growth inhibition of human MDA-MB-231 cells after 96 hrs by ATPlite luminescence assay IC50=1.04 μM	24237195
MDA-MB-435	Growth inhibition assay	96 h	Growth inhibition of human MDA-MB-435 cells after 96 hrs by ATPlite luminescence assay IC50=1.44 μM	24237195
MDA-MB-468	Growth inhibition assay	96 h	Growth inhibition of human MDA-MB-468 cells after 96 hrs by ATPlite luminescence assay IC50=2.73 μM	24237195
MIAPaCa2	Growth inhibition assay	96 h	Growth inhibition of human MIAPaCa2 cells after 96 hrs by ATPlite luminescence assay IC50=0.468 μM	24237195
PANC1	Growth inhibition assay	96 h	Growth inhibition of human PANC1 cells after 96 hrs by ATPlite luminescence assay IC50=1.104 μM	24237195
PC3	Growth inhibition assay	96 h	Growth inhibition of human PC3 cells after 96 hrs by ATPlite luminescence assay IC50=2.16 μM	24237195
T47D	Growth inhibition assay	96 h	Growth inhibition of human T47D cells after 96 hrs by ATPlite luminescence assay IC50=0.649 μM	24237195
SK-N-MC	Growth inhibition assay	96 h	Growth inhibition of human SK-N-MC cells after 96 hrs by ATPlite luminescence assay IC50=0.329 μM	24237195
U87	Growth inhibition assay	96 h	Growth inhibition of human U87 cells after 96 hrs by ATPlite luminescence assay IC50=1.16 μM	24237195
Hs	Growth inhibition assay	96 h	Growth inhibition of human Hs 578T cells after 96 hrs by ATPlite luminescence assay IC50=1.7 μM	24237195
HER218	Growth inhibition assay	96 h	Growth inhibition of human HER218 cells after 96 hrs by ATPlite luminescence assay IC50=0.612 μM	24237195
HCT116	Growth inhibition assay	96 h	Growth inhibition of human HCT116 cells after 96 hrs by ATPlite luminescence assay IC50=0.614 μM	24237195
BT20	Growth inhibition assay	96 h	Growth inhibition of human BT20 cells after 96 hrs by ATPlite luminescence assay IC50=0.489 μM	24237195
BT549	Growth inhibition assay	96 h	Growth inhibition of human BT549 cells after 96 hrs by ATPlite luminescence assay IC50=1.01 μM	24237195
AN3CA	Growth inhibition assay	96 h	Growth inhibition of human AN3CA cells after 96 hrs by ATPlite luminescence assay IC50=0.356 μM	24237195
HCT116	Antiproliferative assay	96 hrs	Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.33 μM.	27524309
MCF7	Antiproliferative assay	72 hrs	Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 0.44 μM.	27524309
DU145	Antiproliferative assay	96 hrs	Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.62 μM.	27524309
HCT116	Antiproliferative assay	72 hrs	Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 0.65 μM.	27524309
MDA-MB-231	Antiproliferative assay	96 hrs	Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.75 μM.	27524309
A2780	Antiproliferative assay	96 hrs	Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.77 μM.	27524309
A549	Antiproliferative assay	96 hrs	Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.83 μM.	27524309
MDA-MB-231	Antiproliferative assay	72 hrs	Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 1.4 μM.	27524309
NCI-H1299	Antiproliferative assay	96 hrs	Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 1.73 μM.	27524309
A2780	Antiproliferative assay	72 hrs	Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 2.14 μM.	27524309
A549	Antiproliferative assay	72 hrs	Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 2.69 μM.	27524309
NCI-H1299	Antiproliferative assay	72 hrs	Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 3.01 μM.	27524309
PC3	Antiproliferative assay	96 hrs	Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 4.45 μM.	27524309
SMMC7721	Antiproliferative assay	96 hrs	Antiproliferative activity against human SMMC7721 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 5.36 μM.	27524309
DU145	Antiproliferative assay	72 hrs	Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 13.08 μM.	27524309
LSD1	Antiproliferative assay	72 hrs	Antiproliferative activity against human SMMC7721 over-expressing LSD1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 15.75 μM.	27524309
PC3	Antiproliferative assay	72 hrs	Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 19.72 μM.	27524309
H460	Antiproliferative assay	48 to 72 hrs	Antiproliferative activity against human H460 cells after 48 to 72 hrs by MTT assay, IC50 = 0.47 μM.	29754076
MCF7	Antiproliferative assay	48 to 72 hrs	Antiproliferative activity against human MCF7 cells after 48 to 72 hrs by MTT assay, IC50 = 0.62 μM.	29754076
Raji	Antiproliferative assay	48 to 72 hrs	Antiproliferative activity against human Raji cells after 48 to 72 hrs by MTT assay, IC50 = 0.98 μM.	29754076
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生物活性

產(chǎn)品描述

靶點(diǎn)

LSD1 ^[1]
(Cell-free assay)

13 nM

體外研究(In Vitro)
體外研究活性	在AML細(xì)胞中，SP2509抑制LSD1與CoREST聯(lián)合，增加啟動(dòng)子特異性H3K4Me3，并誘導(dǎo)p53，p21和C/EBPα。SP250也顯著抑制菌落生長，并誘導(dǎo)OCI-AML3的細(xì)胞凋亡。
激酶實(shí)驗(yàn)	SP2509 活性檢測
激酶實(shí)驗(yàn)	測試化合物在100% DMSO中稀釋至20 ×所需的測試濃度，并將2.5?μL稀釋的藥物樣品加入到黑色384孔板。LSD1酶儲(chǔ)液用測試緩沖液稀釋17倍，將40?μL稀釋的LSD1酶加入到適當(dāng)?shù)目字小Ｈ缓髮⒂衫备^氧化物酶，二甲基K4肽相應(yīng)的組蛋白H3 N端尾部的前21個(gè)氨基酸，和10-乙酰基-3,7-二羥吩惡嗪組成的底物加入孔中。Resorufin在Envision平板閱讀器上以530?nm的激發(fā)波長和595?nm的發(fā)射波長進(jìn)行分析。SP2509對其他氧化酶的活性使用市售試劑盒測定。葡萄糖氧化酶活性(其在擴(kuò)張的構(gòu)象中非共價(jià)結(jié)合FAD)，使用葡萄糖氧化酶試劑盒測定。MAO測定使用MAO-glo試劑盒與MAO-A 和 MAO-B進(jìn)行。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	OCI-AML3，MV4-11 和 MOLM13 細(xì)胞
	濃度	~10 μM
	孵育時(shí)間	96小時(shí)
	方法	培養(yǎng)的AML細(xì)胞用SP2509 和/或PS處理96小時(shí)。在處理結(jié)束時(shí)，細(xì)胞用游離藥物清洗3遍，每種條件下的500個(gè)細(xì)胞接種于甲基纖維素，并在37 °C下培養(yǎng)。菌落形成在接種7–10天后測量。

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/24699304/

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/24699304/

化學(xué)信息&溶解度

分子量	437.90	分子式	C₁₉H₂₀ClN₃O₅S
CAS號(hào)	1423715-09-6	SDF	Download SP2509 SDF
Smiles	CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)C3=C(C=CC(=C3)Cl)O
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 83 mg/mL ( (189.54 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 38 mg/mL ( (86.77 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動(dòng)物體內(nèi)配方計(jì)算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	7.000mg/ml (15.99mM)	以 1 mL 工作液為例,取50μL140mg/ml的澄清DMSO儲(chǔ)備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	10%DMSO 1 90%Corn oil 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	5.000mg/ml (11.42mM)	以 1 mL 工作液為例，取100μL50mg/ml的澄清DMSO儲(chǔ)備液加到900μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	3.500mg/ml (7.99mM)	以 1 mL 工作液為例,取50μL70mg/ml的澄清DMSO儲(chǔ)備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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操作手冊

如果有其他問題，請給我們留言。

* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):