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Neuronal Signaling
Adenosine Deaminase inhibitor
-
DNA/RNA Synthesis inhibitor
Cladribine
僅限科研使用
Cladribine
別名: 2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251 中文名稱：克拉利賓
Cladribine是一種腺苷脫氨酶抑制劑，作用于U266， RPMI8226，和MM1.S細(xì)胞，IC50分別約為2.43 μM， 0.75 μM，和0.18 μM。
Cladribine Chemical Structure
CAS: 4291-63-8
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Cladribine相關(guān)產(chǎn)品
| 相關(guān)化合物庫(kù) | FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 神經(jīng)信號(hào)化合物庫(kù) 血腦屏障通透化合物庫(kù) 抗阿爾茨海默病化合物庫(kù) | 點(diǎn)擊展開(kāi) |
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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| CT26 | Cytotoxicity assay | 3 days | Cytotoxicity against mouse CT26 cells after 3 days by MTT assay, IC50=0.131μM | 21711054 | |
| BT549 | Cytotoxicity assay | 3 days | Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123μM | 21711054 | |
| BV173 | Cytotoxicity assay | 3 days | Cytotoxicity against human BV173 cells after 3 days by MTT assay, IC50=0.0008μM | 21711054 | |
| human SK-UT-1B cells | Proliferation assay | 48 h | Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=1 μM | 25960323 | |
| human MCF7 cells | Proliferation assay | 48 h | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=45 μM | 25960323 | |
| human RPMI8226 cells | Proliferation assay | 48 h | Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM | 25960323 | |
| human KG1 cells | Proliferation assay | 48 h | Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.2 μM | 25960323 | |
| human MOLT3 cells | Proliferation assay | 48 h | Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2.3 μM | 25960323 | |
| human SKHEP1 cells | Proliferation assay | 48 h | Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=4 μM | 25960323 | |
| human K562 cells | Proliferation assay | 48 h | Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=10 μM | 25960323 | |
| human HCT116 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.3 μM | 25462277 | |
| human T47D cells | Cytotoxicity assay | 72 h | Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50=0.7 μM | 25462277 | |
| human HuH7 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay, IC50=1.8 μM | 25462277 | |
| human Raji cells | Cytotoxicity assay | 72 h | Cytotoxicity against human Raji cells after 72 hrs by MTT assay, IC50=0.009 μM | 21840722 | |
| CCRF-CEM cells | Cytotoxicity assay | 72 h | Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM | 21840722 | |
| MES-SA | Cytotoxicity assay | 3 days | Cytotoxicity against human MES-SA cells after 3 days by MTT assay, IC50=0.165μM | 21711054 | |
| K562 | Cytotoxicity assay | 3 days | Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay, IC50=0.17μM | 21711054 | |
| P388D1 | Cytotoxicity assay | 3 days | Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay, IC50=0.285μM | 21711054 | |
| CEM-DNR-bulk | Cytotoxicity assay | 3 days | Cytotoxicity against human CEM-DNR-bulk cells after 3 days by MTT assay, IC50=0.352μM | 21711054 | |
| L1210 | Cytotoxicity assay | 3 days | Cytotoxicity against mouse L1210 cells after 3 days by MTT assay, IC50=0.393μM | 21711054 | |
| EL4 | Cytotoxicity assay | 3 days | Cytotoxicity against mouse EL4 cells after 3 days by MTT assay, IC50=0.848μM | 21711054 | |
| MCF7 | Cytotoxicity assay | 3 days | Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=2.35μM | 21711054 | |
| K562 | Cytotoxicity assay | 3 days | Cytotoxicity against human K562 cells after 3 days by MTT assay, IC50=7.69μM | 21711054 | |
| PC3 | Cytotoxicity assay | 3 days | Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=8.28μM | 21711054 | |
| C6 | Cytotoxicity assay | 3 days | Cytotoxicity against rat C6 cells after 3 days by MTT assay, IC50=9.07μM | 21711054 | |
| HPAC | Cytotoxicity assay | 3 days | Cytotoxicity against human HPAC cells after 3 days by MTT assay, IC50=9.32μM | 21711054 | |
| HCT116 | Cytotoxicity assay | 3 days | Cytotoxicity against human HCT116 cells after 3 days by MTT assay, IC50=9.43μM | 21711054 | |
| HT-29 | Cytotoxicity assay | 3 days | Cytotoxicity against human HT-29 cells after 3 days by MTT assay, IC50=9.44μM | 21711054 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=0.3μM | 28219046 | |
| HuH7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=1.8μM | 28219046 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=2μM | 28219046 | |
| P388 leukemic cell lines | Function assay | In vitro inhibitory effect was tested for cytostatic activity on the growth of lymphoid neoplasm P388 leukemic cell lines, ID50=0.03 μM | 2995666 | ||
| L1210 cell lines | Function assay | In vitro inhibitory effect was tested for cytostatic activity on the growth of murine leukemic L1210 cell lines, ID50=0.03 μM | 2995666 | ||
| L1210 cell lines | Cytotoxicity assay | Compound was tested for cytotoxicity against L1210 cell lines, IC50=0.07 Μm | 1732556 | ||
| HEp-2 cell lines | Cytotoxicity assay | Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.03 μM | 1732556 | ||
| CCRF-CEM cell lines | Cytotoxicity assay | Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM | 1732556 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Cladribine是一種腺苷脫氨酶抑制劑，作用于U266， RPMI8226，和MM1.S細(xì)胞，IC50分別約為2.43 μM， 0.75 μM，和0.18 μM。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | Cladribine主要在淋巴組織中具有活性。 | ||||||
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | Cladribine對(duì)毛細(xì)胞白血病(HCL)，一種慢性B淋巴細(xì)胞增生疾病發(fā)揮顯著的活性，延長(zhǎng)完全緩解期。Cladribine誘導(dǎo)DNA鏈斷裂累積，隨后激活淋巴細(xì)胞中抑癌基因p53。Cladribine可能調(diào)節(jié)MM細(xì)胞中STAT3活性。Cladribine劑量依賴性抑制U266，RPMI8226和MM1.S細(xì)胞的增殖/存活。其中U266對(duì)cladribine敏感性最低，而對(duì)MM1.S敏感性最高。Cladribine治療逐漸增加細(xì)胞周期中G1期的細(xì)胞比例，并減少S期細(xì)胞。Cladribine處理24小時(shí)后似乎能夠增加U266細(xì)胞中G2-M期的比例。在RPMI8226和MM1.S細(xì)胞中都能觀察到cladribine誘導(dǎo)的細(xì)胞凋亡劑量依賴性增加。0.2 μM cladribine治療時(shí)間依賴性顯著誘導(dǎo)MM1.S 中caspase-3，-8，和-9激活和PARP裂解。Cladribine劑量依賴性顯著降低磷酸STAT3 (P-STAT3)水平，但是不影響總STAT3蛋白質(zhì)水平。[1] Cladribine在HSB2細(xì)胞中具有濃度依賴性誘導(dǎo)細(xì)胞凋亡的潛能。[2] Cladribine以劑量依賴的方式抑制原代肥大細(xì)胞(MC)和MC系HMC-1生長(zhǎng)，含有KIT D816V的HMC-1.2細(xì)胞與KIT D816V缺失的HMC-1.1細(xì)胞相比，具有較低的IC50值。[3] Cladribine降低CD14+單核細(xì)胞，以及CD4+和CD8+ T淋巴細(xì)胞的遷移能力。[4] | |||
|---|---|---|---|---|
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | U266，RPMI8226 和 MM1.S | ||
| 濃度 | 0 μM - 32 μM | |||
| 孵育時(shí)間 | 72小時(shí) | |||
| 方法 | 非放射性細(xì)胞增殖試劑盒用于測(cè)定細(xì)胞活性。簡(jiǎn)而言之，人MM細(xì)胞系U266，RPMI8226和MM1.S接種到96孔板，0.1 mL完全培養(yǎng)基(5% FBS)為對(duì)照組，0.1 mL包含一系列劑量cladribine的相同培養(yǎng)基為試驗(yàn)組，培養(yǎng)72小時(shí)。使用微板讀書(shū)器在490 nm下讀取所有孔中的細(xì)胞數(shù)量，每組相對(duì)于100%存活率對(duì)照組的存活細(xì)胞百分?jǐn)?shù)，通過(guò)MTS的減少測(cè)定。 | |||
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Cladribine (0.7-3.5 mM)和/或diltiazem (2.4 mM)，腹腔注射到成年斑馬魚(yú)，通過(guò)HPLC分析心血管健康的潛在標(biāo)志物，紅血球(RBC)裂解物嘌呤核苷酸(例如ATP)的水平。Diltiazem增加RBC ATP濃度，該作用被共注射cladribine所抑制。[5] Ia 和s.c.給藥后，伴隨雙相下降，Cladribine血漿濃度急速減少。單劑Cladribine 以1 mg/kg ia 和 2 mg/kg s.c. 注射后，AUC和t 1/2β分別為0.66: 1.2 μg ×h/mL和3.5: 4.5小時(shí)。[6] | |
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 成年野生型(AB)斑馬魚(yú) |
| Dosages | 0.7 mM - 3.5?mM | |
| Administration | 腹腔注射給藥 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05797740 | Recruiting | Multiple Sclerosis |
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany |
August 3 2023 | -- |
| NCT04997148 | Completed | Relapsing-Remitting Multiple Sclerosis |
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany |
August 11 2021 | -- |
|
化學(xué)信息&溶解度
| 分子量 | 285.69 | 分子式 | C10H12ClN5O3 |
| CAS號(hào) | 4291-63-8 | SDF | Download Cladribine SDF |
| Smiles | C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O | ||
| 儲(chǔ)存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 57 mg/mL ( (199.51 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
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體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)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 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)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(qǐng)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(guò)該批次藥物DMSO溶解度，請(qǐng)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。
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