- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實驗
- Cell Counting Kit-8 (CCK-8)
- 新產(chǎn)品
- 聯(lián)系我們
Serdemetan (JNJ-26854165)
Serdemetan (JNJ-26854165)是一種HDM2泛素連接酶拮抗劑，作用于p53野生型細(xì)胞，誘導(dǎo)早期凋亡，在缺乏功能性p53的細(xì)胞中，抑制細(xì)胞增殖而延遲細(xì)胞凋亡。
Serdemetan (JNJ-26854165) Chemical Structure
CAS: 881202-45-5
產(chǎn)品質(zhì)控
批次：
S117202
DMSO]66 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false
純度：
99.58%
99.58
Serdemetan (JNJ-26854165)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| KU-19-19 cell | Growth inhibition assay | Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=0.93236 μM | SANGER | ||
| H4 cell | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50=1.06707 μM | SANGER | ||
| KGN cell | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay, IC50=1.6205 μM | SANGER | ||
| 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM | SANGER | ||
| 769-P cell | Growth inhibition assay | Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM | SANGER | ||
| K5 cell | Growth inhibition assay | Inhibition of human K5 cell growth in a cell viability assay, IC50=2.01624 μM | SANGER | ||
| MLMA cell | Growth inhibition assay | Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=2.03217 μM | SANGER | ||
| MLMA cell | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay, IC50=2.28703 μM | SANGER | ||
| EW-7 cell | Growth inhibition assay | Inhibition of human EW-7 cell growth in a cell viability assay, IC50=2.32695 μM | SANGER | ||
| SW1088 cell | Growth inhibition assay | Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.80651 μM | SANGER | ||
| MC-IXC cell | Growth inhibition assay | Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=2.87792 μM | SANGER | ||
| NCI-H2052 cell | Growth inhibition assay | Inhibition of human NCI-H2052 cell growth in a cell viability assay, IC50=3.08157 μM | SANGER | ||
| IGR-1 cell | Growth inhibition assay | Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=3.12028 μM | SANGER | ||
| DSH1 cell | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50=3.24296 μM | SANGER | ||
| PA-1 cell | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.30059μM | SANGER | ||
| SK-MEL-3 cell | Growth inhibition assay | Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=3.31207 μM | SANGER | ||
| SW900 cell | Growth inhibition assay | Inhibition of human SW900 cell growth in a cell viability assay, IC50=3.48255 μM | SANGER | ||
| CAKI-1 cell | Growth inhibition assay | Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=3.52738 μM | SANGER | ||
| ES1 cell | Growth inhibition assay | Inhibition of human ES1 cell growth in a cell viability assay, IC50=3.52897 μM | SANGER | ||
| SK-N-DZ cell | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=3.62595 μM | SANGER | ||
| RH-1 cell | Growth inhibition assay | Inhibition of human RH-1 cell growth in a cell viability assay, IC50=3.68463 μM | SANGER | ||
| ES8 cell | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay, IC50=3.69702 μM | SANGER | ||
| NEC8 cell | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay, IC50=3.76982 μM | SANGER | ||
| LNCaP-Clone-FGC cell | Growth inhibition assay | Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=3.83536 μM | SANGER | ||
| HCE-4 cell | Growth inhibition assay | Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=3.9807 μM | SANGER | ||
| U-118-MG cell | Growth inhibition assay | Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=4.01066 μM | SANGER | ||
| GI-ME-N cell | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=4.08796 μM | SANGER | ||
| LB1047-RCC cell | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=4.16143 μM | SANGER | ||
| HT-1080 cell | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=4.19921 μM | SANGER | ||
| NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=4.35047 μM | SANGER | ||
| NCI-H1693 cell | Growth inhibition assay | Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50=4.44895 μM | SANGER | ||
| HSC-3 cell | Growth inhibition assay | Inhibition of human HSC-3 cell growth in a cell viability assay, IC50=4.49933 μM | SANGER | ||
| MDA-MB-231 cell | Growth inhibition assay | Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=4.55899 μM | SANGER | ||
| HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay, IC50=4.7863 μM | SANGER | ||
| BT-549 cell | Growth inhibition assay | Inhibition of human BT-549 cell growth in a cell viability assay, IC50=4.7887 μM | SANGER | ||
| NB17 cell | Growth inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay, IC50=4.78976 μM | SANGER | ||
| 5637 cell | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM | SANGER | ||
| OVCAR-8 cell | Growth inhibition assay | Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50=4.92436 μM | SANGER | ||
| G-402 cell | Growth inhibition assay | Inhibition of human G-402 cell growth in a cell viability assay, IC50=4.93035 μM | SANGER | ||
| BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=5.07218 μM | SANGER | ||
| HCC1806 cell | Growth inhibition assay | Inhibition of human HCC1806 cell growth in a cell viability assay, IC50=5.08339 μM | SANGER | ||
| COLO-800 cell | Growth inhibition assay | Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=5.1264 μM | SANGER | ||
| FADU cell | Growth inhibition assay | Inhibition of human FADU cell growth in a cell viability assay, IC50=5.36557 μM | SANGER | ||
| NCI-H1651 cell | Growth inhibition assay | Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=5.39409 μM | SANGER | ||
| AGS cell | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50=5.47711 μM | SANGER | ||
| CHP-212 cell | Growth inhibition assay | Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=5.39409 μM | SANGER | ||
| YAPC cell | Growth inhibition assay | Inhibition of human YAPC cell growth in a cell viability assay, IC50=5.47711 μM | SANGER | ||
| GOTO cell | Growth inhibition assay | Inhibition of human GOTO cell growth in a cell viability assay, IC50=5.49576 μM | SANGER | ||
| KYSE-510 cell | Growth inhibition assay | Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=5.511 μM | SANGER | ||
| NCI-H2342 cell | Growth inhibition assay | Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=5.53278 μM | SANGER | ||
| BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.62835 μM | SANGER | ||
| EW-16 cell | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay, IC50=5.72093 μM | SANGER | ||
| SK-MEL-30 cell | Growth inhibition assay | Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=5.74543 μM | SANGER | ||
| HLE cell | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=5.77489 μM | SANGER | ||
| T98G cell | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50=5.79635 μM | SANGER | ||
| HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=5.84228 μM | SANGER | ||
| NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.94766 μM | SANGER | ||
| SW780 cell | Growth inhibition assay | Inhibition of human SW780 cell growth in a cell viability assay, IC50=5.96949 μM | SANGER | ||
| KYSE-180 cell | Growth inhibition assay | Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=5.97654 μM | SANGER | ||
| MDA-MB-361 cell | Growth inhibition assay | Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=5.98647 μM | SANGER | ||
| SNU-C2B cell | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=6.01138 μM | SANGER | ||
| NCI-H661 cell | Growth inhibition assay | Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=6.0694 μM | SANGER | ||
| OE33 cell | Growth inhibition assay | Inhibition of human OE33 cell growth in a cell viability assay, IC50=6.14389 μM | SANGER | ||
| TYK-nu cell | Growth inhibition assay | Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=6.21863 μM | SANGER | ||
| COLO-792 cell | Growth inhibition assay | Inhibition of human COLO-792 cell growth in a cell viability assay, IC50=6.25219 μM | SANGER | ||
| HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay, IC50=6.2676 μM | SANGER | ||
| D-566MG cell | Growth inhibition assay | Inhibition of human D-566MG cell growth in a cell viability assay, IC50=6.33491 μM | SANGER | ||
| U031 cell | Growth inhibition assay | Inhibition of human U031 cell growth in a cell viability assay, IC50=6.41816 μM | SANGER | ||
| COR-L23 cell | Growth inhibition assay | Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=6.43346 μM | SANGER | ||
| NCI-H2452 cell | Growth inhibition assay | Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=6.52281 μM | SANGER | ||
| BB65-RCC cell | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=6.6459 μM | SANGER | ||
| CAL-33 cell | Growth inhibition assay | Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=6.65665 μM | SANGER | ||
| 點擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Serdemetan (JNJ-26854165)是一種HDM2泛素連接酶拮抗劑，作用于p53野生型細(xì)胞，誘導(dǎo)早期凋亡，在缺乏功能性p53的細(xì)胞中，抑制細(xì)胞增殖而延遲細(xì)胞凋亡。 | |||
|---|---|---|---|---|
| 特性 | JNJ 26854165是口服生物有效性的，小分子HDM2拮抗劑，具有有效的抗腫瘤活性。 | |||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | JNJ-26854165是新型激活p53的色胺衍生物，作為HDM2泛素連接酶拮抗劑。JNJ-26854165作用于白血病細(xì)胞系，抑制細(xì)胞生長，且誘導(dǎo)凋亡，作用于OCI-AML-3, MOLM-13,NALM-6和REH細(xì)胞72小時后，IC50值分別為0.24,0.33,0.32和0.44 μM。此外, JNJ-26854165作用于p53突變的細(xì)胞，加速蛋白酶調(diào)節(jié)的p21降解和抗p53對p21的轉(zhuǎn)錄誘導(dǎo), 誘導(dǎo)S期延遲，且上調(diào)E2F1表達, 導(dǎo)致S期細(xì)胞優(yōu)先凋亡。[1] JNJ-26854165是口服MDM2抑制劑，可以抑制MDM2-p53復(fù)合體與蛋白酶的相互作用，且通過與MDM2的RING域結(jié)合提高p53水平。[2]最新研究顯示JNJ-26854165作用于四種人類癌細(xì)胞系:H460,A549,p53-WT-HCT116,和p53-null-HCT116，抑制無性繁殖生存。[3] | |||
|---|---|---|---|---|
| 細(xì)胞實驗 | 細(xì)胞系 | OCI-AML-3,MOLM-13,NB4和U937細(xì)胞 | ||
| 濃度 | 0到10 μM | |||
| 孵育時間 | 72 小時 | |||
| 方法 | 細(xì)胞系維持在含10%熱滅活胎牛血清(FCS)的RPMI 1640培養(yǎng)基上。急性骨髓性白血病(AML) 患者體內(nèi)得到的OCI-AML-3, MOLM-13, NB4和 U937 細(xì)胞,慢性髓細(xì)胞性白血病(CML)患者體內(nèi)得到的K562細(xì)胞,急性成淋巴細(xì)胞性白血病(ALL)患者體內(nèi)得到的NALM-6, REH, P12-ICHIKAWA和PF-382細(xì)胞。OCI-AML-3, MOLM-13, NALM-6和 REH 細(xì)胞具有野生型p53, 然而NB4,U937,K562,P12-ICHIKAWA和PF-382細(xì)胞具有突變型p53，獲得對數(shù)生長期細(xì)胞系，接種，用JNJ-26854165處理。白血病患者體內(nèi)獲得的白血病細(xì)胞中獲得肝素外周血或骨髓樣本。通過密度梯度離心純化單核細(xì)胞，非黏著細(xì)胞懸浮在含10%FCS的RPMI 1640培養(yǎng)基上。正常骨髓衍生的干細(xì)胞接種在含MEM-α培養(yǎng)基的12孔板上，24小時后，加入AML細(xì)胞。為了研究骨髓干細(xì)胞作用于原代白血病細(xì)胞的效果，培養(yǎng)AML 細(xì)胞。在JNJ-26854165和 AraC的聯(lián)合實驗中,用0,2,5或 10 μM。JNJ-26854165 處理AML細(xì)胞系。在OCI-AML-3細(xì)胞中 JNJ-26854165與 AraC的濃度比為1:1，在其他細(xì)胞中為10:1。兩種試劑同時加到細(xì)胞中，培養(yǎng)48小時。JNJ-26854165和Doxorubicin聯(lián)用的實驗中,兩種試劑同時加到細(xì)胞中，培養(yǎng)48小時。用 0, 25, 50或 100 nM Doxorubicin處理細(xì)胞 (用0,100,200 或400 nM Doxorubicin 處理OCI-AML-3細(xì)胞和原代白血病細(xì)胞)，Doxorubicin 與JNJ-26854165 的濃度比為1:10 (在OCI-AML-3細(xì)胞和原代白血病細(xì)胞中比為1:25)。通過臺酚藍染料重復(fù)計數(shù)，測評細(xì)胞活力。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3 MDM2 / p-MDM2 / p53 ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR p53 / HDM2 / HDMX / p21 / Noxa / Puma |
|
27999193 | |
| Growth inhibition assay | Cell viability |
|
23820125 | |
| Immunofluorescence | p53 |
|
27999193 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | JNJ-26854165按20 mg/kg劑量口服飼喂于三十六分之十七(47%)實體移植瘤和七分之五(71%) ALL移植瘤，持續(xù)5天，重復(fù)進行6周，導(dǎo)致EFS分布出現(xiàn)明顯區(qū)別。[4] | |
|---|---|---|
| 動物實驗 | Animal Models | 皮下注射kidney/rhabdoid腫瘤,肉瘤, 成神經(jīng)細(xì)胞瘤, 和非惡性膠質(zhì)瘤腦癌的雌性CB17SC scid-/-小鼠，攜帶神經(jīng)膠質(zhì)瘤的BALB/c nu/nu小鼠 |
| Dosages | ≤20 mg/kg | |
| Administration | 口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00676910 | Completed | Neoplasms |
Johnson & Johnson Pharmaceutical Research & Development L.L.C. |
November 2006 | Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 328.41 | 分子式 | C21H20N4 |
| CAS號 | 881202-45-5 | SDF | Download Serdemetan (JNJ-26854165) SDF |
| Smiles | C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 66 mg/mL ( (200.96 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 2 mg/mL (6.08 mM) Water : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解度 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 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(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。
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