Lenalidomide
别名: CC-5013 中文名称：来那度胺
Lenalidomide是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。
Lenalidomide Chemical Structure
CAS: 191732-72-6
产品质控
批次：
纯度：
99.99%
99.99
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| DF15 | Function assay | 0.1 to 10 uM | 5 hrs | Induction of cereblon-mediated aiolos degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis | 28425720 |
| OPM2 | Function assay | 0.1 to 10 uM | 5 hrs | Induction of cereblon-mediated aiolos degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis | 28425720 |
| DF15 | Function assay | 0.1 to 10 uM | 5 hrs | Induction of cereblon-mediated ikaros degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis | 28425720 |
| OPM2 | Function assay | 0.1 to 10 uM | 5 hrs | Induction of cereblon-mediated ikaros degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis | 28425720 |
| EC9706 | Antiproliferative assay | 150 ug/mL | 48 hrs | Antiproliferative activity against human EC9706 cells at 150 ug/mL after 48 hrs by CCK-8 assay | 28757066 |
| DF15 | Function assay | 4 hrs | Induction of CRL4/CRBN ubiquitin ligase-mediated aiolos degradation in human DF15 cells expressing pLOC-ePL-tagged aiolos after 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay, EC50 = 0.053 μM. | 28358507 | |
| DF15 | Function assay | 4 hrs | Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing ePL-tagged ikaros after 4 hrs by luminometric analysis, EC50 = 0.067 μM. | 28425720 | |
| DF15 | Function assay | 4 hrs | Induction of cereblon-mediated aiolos degradation in human DF15 cells expressing ePL-tagged aiolos after 4 hrs by luminometric analysis, EC50 = 0.087 μM. | 28425720 | |
| T-cells | Function assay | 2 to 3 days | Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA, EC50 = 0.15 μM. | 23168019 | |
| NAMALWA | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.36 μM. | 23168019 | |
| CD34+ progenitor cells | Function assay | 14 days | Decrease in erythroid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as CD36 expression after 14 days | 17576924 | |
| CD34+ progenitor cells | Function assay | 14 days | Decrease in myeloid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as CD33 expression after 14 days | 17576924 | |
| CD34+ progenitor cells | Function assay | 14 days | Decrease in erythroid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as glycophorin A expression after 14 days | 17576924 | |
| CD34+ progenitor cells | Growth inhibition assay | 14 days | Inhibition of cell proliferation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient after 14 days | 17576924 | |
| CD34+ progenitor cells | Growth inhibition assay | 14 days | Growth inhibition of CD34+ progenitor cells from non-del(5q) myelodysplastic syndrome patient after 14 days | 17576924 | |
| A2780 | Growth Inhibition Assay | IC50=35.3601 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=34.7443 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=32.9568 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=32.683 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=31.6755 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=31.2274 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=31.1614 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=30.8839 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=30.7346 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=30.33 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=30.3099 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=29.7317 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=29.6974 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=28.2026 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=25.5407 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=25.4009 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=25.0149 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=23.8696 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=22.6963 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=22.1563 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=20.5759 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=20.3573 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=19.9076 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=17.9968 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=17.783 μM | SANGER | ||
| HSC-4 | Growth Inhibition Assay | IC50=17.6601 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=17.143 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=16.626 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=16.5297 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=16.4652 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=16.1486 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=15.499 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=15.3979 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=14.9108 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=14.5796 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=14.4892 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=14.2473 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=13.8199 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=13.48 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=13.2099 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=12.6241 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=11.9764 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=11.571 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=11.4467 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=10.0172 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=8.67585 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=7.89512 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=6.21849 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=4.10515 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=2.97001 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=2.92212 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=2.15038 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=35.7681 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=36.2137 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=37.4212 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=38.3885 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=39.7789 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=40.4746 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=41.2069 μM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=41.9871 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=43.7917 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=44.2776 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=46.6986 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=48.3224 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=50.3545 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=52.3142 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=52.7024 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=52.8559 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=53.0508 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=53.6364 μM | SANGER | ||
| LU-135 | Growth Inhibition Assay | IC50=55.1853 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=55.818 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=55.9489 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=56.2893 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=56.3204 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=57.0142 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=57.5705 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=58.6264 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=58.826 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=58.8643 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=58.8942 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=59.091 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=59.2809 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=59.6287 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=60.449 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=60.9905 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=61.0786 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=61.5333 μM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=61.875 μM | SANGER | ||
| NCI-H1993 | Growth Inhibition Assay | IC50=63.4043 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=65.0121 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=65.988 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=67.0798 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=67.4948 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=69.8314 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=70.1243 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=70.9395 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=71.172 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=71.4434 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=71.965 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=72.9702 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=73.1489 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=74.7486 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=74.9308 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=75.7663 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=78.6147 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=78.9939 μM | SANGER | ||
| COLO-680N | Growth Inhibition Assay | IC50=79.1007 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=79.812 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=81.1187 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=81.7296 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=81.8849 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=82.4134 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=83.0033 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=83.2575 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=85.4912 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=85.7908 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=86.2032 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=86.4336 μM | SANGER | ||
| SW900 | Growth Inhibition Assay | IC50=87.2053 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=87.2243 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=91.0405 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=91.6374 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=92.0219 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=92.7697 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=92.8821 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=93.1 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=93.8462 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=94.3055 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=96.0516 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lenalidomide是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | CC-5013强诱导IL-2和sIL-2R产量。CC-5013作用于T细胞，诱导CD28的酪氨酸磷酸化，随后下调NF-κB的激活。[2] Lenalidomide和Pomalidomide作用于表达与Thalidomide结合野生型CRBN的，而不是Thalidomide结合缺陷型CRBN(YW/AA)的HEK293 T细胞，抑制CRBN自体泛素化。KMS12多发性骨髓瘤细胞中，CRBN野生型蛋白而不是CRBN(YW/AA) 突变型蛋白的过表达, 放大Pomalidomide调节的c-myc和IRF4表达降低和p21(WAF-1) 表达增高。H929 多发性骨髓瘤细胞系中长期抗Lenalidomide 的选择性与CRBN降低相关,然而抗Pomalidomide和 Lenalidomide的DF15R多发性骨髓瘤 中, 检测不到CRBN蛋白。[3] Lenalidomide通过下调肿瘤细胞抑制性分子表达而抑制缺陷发生。Lenalidomide防止肿瘤诱导的T细胞裂解功能障碍发生。Lenalidomide 作用于T细胞，抑制慢性淋巴细胞性白血病（CLL）细胞诱导的T细胞肌动蛋白突触功能受损, 且下调CLL抑制配体及其他受体的表达。Lenalidomide 作用于FL, DLBCL, HL, MM, SCC,和 OC，抑制肿瘤诱导的免疫抑制，且作用于所有检测的肿瘤细胞时,下调免疫抑制配体表达。[4] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | 良性或恶性 B (CLL)细胞, RPMI8226 MM 细胞 | ||
| 浓度 | 1 μM或5 nM | |||
| 孵育时间 | 24小时 | |||
| 方法 | 使用CellTracker Blue CMAC对良性或恶性B (CLL)细胞(2 × 106)进行染色， 然后使用2 μg/mL金黄色葡萄球菌超抗原(sAg) (SEA 和 SEB) 在37oC下进行脉冲处理30分钟。B细胞和等量T细胞(从原代共培养中纯化的)按200 × g转速离心5分钟，然后与CD8+ T 细胞在37oC下温育10分钟，或者与 CD3+ T细胞温育20分钟。使用细胞收集器使细胞转移到显微镜载玻片上，然后在室温下和3% 溶于PBS的甲醛混合15分钟。在完全培养基中加入终浓度为1 μM的Lenalidomide。对照组则使用DMSO处理细胞。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | phospho-IKKβ / IKKβ MDM2 / p-MDM2 / p-p53 / p53 |
|
22698399 | |
| Growth inhibition assay | Cell viability |
|
22698399 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 口服处理Lenalidomide，显著抑制bFGF诱导的血管生成，这种作用存在剂量依赖性。Lenalidomide 显著降低血管面积百分数，从对照组的5.16%降低到实验组的2.58（50 mg/kg剂量处理）和 1.69（250 mg/kg 剂量处理）。 Lenalidomide 显著降低全部MVL，从对照组的21.07降低到实验组的8.11（50 mg/kg剂量处理）和1.90（250 mg/kg剂量处理）。[5] |
|
|---|---|---|
| 动物实验 | Animal Models | 携带HUVECs细胞的成年雄性Sprague–Dawley大鼠 |
| Dosages | 50 mg/kg和250 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06177028 | Not yet recruiting | Cognitive Impairment Mild|Cognitive Dysfunction|Amyloid Plaque|Neurodegenerative Disease Hereditary|Inflammation Brain |
St. Joseph''s Hospital and Medical Center Phoenix|Texas Tech University |
January 2 2024 | Phase 2 |
| NCT06149286 | Recruiting | Relapsed/Refractory Follicular Lymphoma|Marginal Zone Lymphoma (MZL) |
Regeneron Pharmaceuticals |
December 28 2023 | Phase 3 |
| NCT06299553 | Recruiting | DLBCL - Diffuse Large B Cell Lymphoma |
Incyte Biosciences Italy S.r.l |
December 4 2023 | -- |
化学信息&溶解度
| 分子量 | 259.26 | 分子式 | C13H13N3O3 |
| CAS号 | 191732-72-6 | SDF | Download Lenalidomide SDF |
| Smiles | C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 52 mg/mL ( (200.57 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
What is the formulation for mouse injection(i.p.)?
回答：
This paper has the information you need: http://link.springer.com/article/10.1208/s12248-012-9401-2. Add lenalidomide to the appropriate volume of sterile phosphate-buffered saline (PBS) containing 1% hydrochloric acid (HCl). the pH of this preparation was adjusted to 7.0–7.6 using sodium hydroxide and sterile filtered using a 0.22 μm Steriflip filter.
问题 2:
what is the procedure to resuspend this compound？
回答：
You can resuspend this compund by DMSO, the solubility is about 52 mg/mL (200.57 mM). For in vivo study, you can prepare the working solution with the vehicle of: 30% PEG400/0.5% Tween80/5% propylene glycol for oral administration.
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