Thalidomide
Based on 26 publication(s) in Google Scholar
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 50-35-1
- Fòrmula: C13H10N2O4
- Peso molecular:258.23
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Thalidomide
More- Nat Cancer. 2022 May;3(5):595-613. [Abstract]
- Cell Stem Cell. 2026 May 15:S1934-5909(26)00158-X. [Abstract]
- Nat Commun. 2022 Sep 10;13(1):5324. [Abstract]
- Nat Commun. 2017 May 22:8:15398. [Abstract]
- Acta Pharm Sin B. 2024 Aug;14(8):3493-3512. [Abstract]
- Aggregate. 2025 Oct 12.
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- J Hazard Mater. 2026 Mar 1:505:141552. [Abstract]
- Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254. [Abstract]
- J Med Chem. 2025 Oct 23;68(20):21172-21186. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Sci Rep. 2024 Dec 28;14(1):31445. [Abstract]
- Oncol Rep. 2022 Oct;48(4):169. [Abstract]
- ACS Pharmacol Transl Sci. 2021 Feb 26;4(2):941-952. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Food Chem Toxicol. 2022 Nov:169:113441. [Abstract]
- J Appl Toxicol. 2022 Mar;42(3):380-391. [Abstract]
- Charles University. 2026.
- SSRN. 2025 Dec 15.
- Chemrxiv. 2025 Nov 17.
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- bioRxiv. 2025 Jun 19.
- bioRxiv. 2023 Jun 28.
- Elife. 2018 Aug 1:7:e38430. [Abstract]
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Actividad biológica
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Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
176.11 μM
Compound: Tha
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Antiproliferative activity against mouse 4T1 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
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[PMID: 37376788] |
| DLD-1 | IC50 |
>50 μM
Compound: Thalidomide
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Cytotoxicity against human DLD1 cells by MTT assay
Cytotoxicity against human DLD1 cells by MTT assay
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[PMID: 19394719] |
| EA.hy 926 | IC50 |
200 μM
Compound: Thalidomide
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Antiproliferative activity against human EAhy926 cells
Antiproliferative activity against human EAhy926 cells
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[PMID: 19103485] |
| Ehrlich | IC50 |
0.26 nM
Compound: Thalidomide
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Cytotoxicity against mouse Ehrlich cells assessed as cell growth inhibition incubated for 3 hrs by trypan blue exclusion assay
Cytotoxicity against mouse Ehrlich cells assessed as cell growth inhibition incubated for 3 hrs by trypan blue exclusion assay
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[PMID: 34710743] |
| Ehrlich | IC50 |
2.6 x 10-4 μM
Compound: Thalidomide
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Cytotoxicity against mouse Ehrlich cells assessed as cell growth inhibition incubated for 3 hrs by trypan blue exclusion assay
Cytotoxicity against mouse Ehrlich cells assessed as cell growth inhibition incubated for 3 hrs by trypan blue exclusion assay
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[PMID: 34710743] |
| HeLa | IC50 |
2.04 μM
Compound: thalidomide
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Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation
Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation
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[PMID: 17845850] |
| HL-60 | IC50 |
>50 μM
Compound: Thalidomide
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Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
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[PMID: 19394719] |
| HT-29 | IC50 |
>50 μM
Compound: Thalidomide
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Cytotoxicity against human HT-29 cells by MTT assay
Cytotoxicity against human HT-29 cells by MTT assay
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[PMID: 19394719] |
| HUVEC | IC50 |
>50 μM
Compound: Thalidomide
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Cytotoxicity against HUVEC by MTT assay
Cytotoxicity against HUVEC by MTT assay
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[PMID: 19394719] |
| KMS-12-PE | IC50 |
>75 μM
Compound: 1
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Antiproliferative activity against human KMS-12-PE cells assessed as inhibition of cell proliferation incubated for 48 hrs by CellTiter Glo luminescence based MTT assay
Antiproliferative activity against human KMS-12-PE cells assessed as inhibition of cell proliferation incubated for 48 hrs by CellTiter Glo luminescence based MTT assay
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[PMID: 36476642] |
| MOLP-8 | IC50 |
>75 μM
Compound: 1
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Antiproliferative activity against human MOLP8 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CellTiter Glo luminescence based MTT assay
Antiproliferative activity against human MOLP8 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CellTiter Glo luminescence based MTT assay
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[PMID: 36476642] |
| PBMC | IC50 |
77 μM
Compound: 3
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Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA
Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA
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[PMID: 23168019] |
| PBMC | IC50 |
~ 200 μM
Compound: Thalidomide
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Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC
Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC
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[PMID: 9873600] |
| ST486 | IC50 |
>50 μM
Compound: Thalidomide
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Cytotoxicity against human ST486 cells by MTT assay
Cytotoxicity against human ST486 cells by MTT assay
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[PMID: 19394719] |
| T-cell | EC50 |
>10 μM
Compound: 3
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Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA
Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA
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[PMID: 23168019] |
| THP-1 | IC50 |
>2 nM
Compound: 1
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Inhibition of LPS-induced Tumor necrosis factor-alpha production (TNF-alpha) in THP-1 cells
Inhibition of LPS-induced Tumor necrosis factor-alpha production (TNF-alpha) in THP-1 cells
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[PMID: 9871710] |
| U-937 | IC50 |
>500 μM
Compound: Thalidomide
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Inhibition of PDE4 enzyme from U937 cells
Inhibition of PDE4 enzyme from U937 cells
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[PMID: 9873600] |
| WI-38 | IC50 |
>100 μg/mL
Compound: 10 (Thalidomide)
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The cytotoxicity assessed using human embryonic lung fibroblast WI-38 cells.
The cytotoxicity assessed using human embryonic lung fibroblast WI-38 cells.
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[PMID: 9288167] |
Thalidomide has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, and targets cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM[1].
Thalidomide (50 μg/mL) potentiates the anti-tumor activity of Icotinib against the proliferation of both PC9 and A549 cells, and this effect is correlated with apoptosis and cell migration. In addition, Thalidomide and Icotinib inhibits the EGFR and VEGF-R2 pathways in PC9 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Thalidomide (200 mg/kg, p.o.) combined with Icotinib shows synergistic anti-tumor effects in nude mice bearing PC9 cells, suppressing tumor growth and promoting tumor death[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 50-35-1
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Appearance Solid
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Peso molecular 258.23
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Fòrmula C13H10N2O4
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Color White to off-white
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C3=CC=CC=C31)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (26)
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Journal Impact Factor
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Most Recent
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Nat Cancer
IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia. [Abstract]2022 May;3(5):595-613. PMID: 35534777
Thalidomide purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 May;3(5):595-613. [Abstract]
Western blot analysis for IKAROS, CK1α and MENIN protein following treatment of MV4;11 human MLL-r AML cell line for 5 hours with increasing doses of Thalidomide, lenalidomide, Pomalidomide and iberdomide (10,100, 1000 nM), using ACTIN as a loading control.
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Cell Stem Cell
Human PSC-derived sinoatrial node-cardiac plexus assembloids model innervation-associated maturation of pacemaker systems. [Abstract]2026 May 15:S1934-5909(26)00158-X. PMID: 42143017 -
Nat Commun
Functional genomics uncovers the transcription factor BNC2 as required for myofibroblastic activation in fibrosis. [Abstract]2022 Sep 10;13(1):5324. PMID: 36088459
Thalidomide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 10;13(1):5324. [Abstract]
Western immunoassays used to monitor changes in BNC2 levels in LX2 cells treated with 1 μM pomalidomide (Pom.), thalidomide (Thal.), CC-885, Iberdomide (Iber.) or vehicle for 24 h.
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Nat Commun
pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase. [Abstract]2017 May 22:8:15398. PMID: 28530236
Thalidomide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 May 22:8:15398. [Abstract]
HEK293T cells are treated with 50 μg/mL Cycloheximide and increasing concentrations of Lenalidomide, Thalidomide or with DMSO, and cells are incubated for 6 h. ZFP91 and GAPDH levels are detected using anti-ZFP91 or anti-GAPDH immunoblotting.
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Acta Pharm Sin B
Phenylalanine deprivation inhibits multiple myeloma progression by perturbing endoplasmic reticulum homeostasis. [Abstract]2024 Aug;14(8):3493-3512. PMID: 39220878 -
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Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 15;6(4):102053. PMID: 40187357 -
Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
J Hazard Mater
A new mechanism for ubiquitination in polystyrene nanoplastic-induced spatial cognitive dysfunction through microglial activation-induced apoptosis of neurons. [Abstract]2026 Mar 1:505:141552. PMID: 41734560 -
Acta Pharmacol Sin
The novel cereblon modulator CC-885 inhibits mitophagy via selective degradation of BNIP3L. [Abstract]2020 Sep;41(9):1246-1254. PMID: 32210356 -
J Med Chem
Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity. [Abstract]2025 Oct 23;68(20):21172-21186. PMID: 41066447 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Sci Rep
Identifying novel aging-related diagnostic and prognostic models and aging-targeted drugs for sepsis patients. [Abstract]2024 Dec 28;14(1):31445. PMID: 39732977 -
Oncol Rep
Synergistic effects of thalidomide and cisplatin are mediated via the PI3K/AKT and JAK1/STAT3 signaling pathways in cervical cancer. [Abstract]2022 Oct;48(4):169. PMID: 35920185 -
ACS Pharmacol Transl Sci
General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex. [Abstract]2021 Feb 26;4(2):941-952. PMID: 33860212 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Food Chem Toxicol
Melatonin attenuates chronic stress-induced hippocampal inflammatory response and apoptosis by inhibiting ADAM17/TNF-α axis. [Abstract]2022 Nov:169:113441. PMID: 36162616 -
J Appl Toxicol
2022 Mar;42(3):380-391. PMID: 34322893 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
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Elife
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. [Abstract]2018 Aug 1:7:e38430. PMID: 30067223
Thalidomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1:7:e38430. [Abstract]
H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.
Thalidomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1:7:e38430. [Abstract]
Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.
Solvente y solubilidad
DMSO : 100 mg/mL (387.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
THP-1 cells, A549 cells and KYSE30 cells are cultured in RPMI-1640 Medium supplemented with 10% fetal bovine serum and maintained at 37 °C in an atmosphere of 5% CO2 and 95% room air. THP-1 cells is irradiated with a single dose of 4 Gy 6-MV X-ray and treated with or without Thalidomide (0.2 μmol/mL)-containing medium for 48 h after radiation. The concentration of Thalidomide is selected based on the preliminary results[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
A total of 24 WT C57BL/6 mice are randomly divided into 4 groups for the experiments (n = 6 in each group): a control group, an irradiated group, a group irradiated along with Thalidomide, and a Thalidomide only group. Based on the preliminary results, 100 mg/kg Thalidomide is used in the experiment. Thalidomide is dissolved in DMSO vehicle. The treatment group receives the indicated dose of Thalidomide in 200 μL by gavage every other day beginning on day 1 for six treatments. The control mice receives 200 μL 0.1% DMSO contained-saline only. The lungs are harvested at 12 weeks after irradiation for the analysis. A total of 20 Nrf2-/- mice are randomly divided into 4 groups for the experiments (n = 5 in each group). The experiment procedures of Nrf2-/- mice are the same as WT C57BL/6 mice. In addition, a total of 30 WT C57BL/6 mice are randomly divided into 5 groups for the subsequent experiments (n = 6 in each group): a control group, an irradiated group, a group irradiated along with CDDO-Me and Thalidomide, a group irradiated along with CDDO-Me, and a group irradiated along with Thalidomide. 600 ng and 100 mg/kg are selected as the dose of CDDO-Me and Thalidomide for the experiment, respectively. The treatment group receives the indicated dose of CDDO-Me or Thalidomide in 200 μL by gavage every other day beginning on day 1 for six times. For the combined group of CDDO-Me and Thalidomide, CDDO-Me is delivered in 200 μL by gavage every other day beginning on day 1 for six treatments. Thalidomide is delivered in 200 μL by gavage every other day beginning on day 2 for six treatments[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Fischer ES, et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014 Aug 7;512(7512):49-53. [Content Brief]
[2]. Sun X, et al. Synergistic Inhibition of Thalidomide and Icotinib on Human Non-Small Cell Lung Carcinomas Through ERK and AKT Signaling. Med Sci Monit. 2018 May 15;24:3193-3203. [Content Brief]
[3]. Bian C, et al. Thalidomide (THD) alleviates radiation induced lung fibrosis (RILF) via down-regulation of TGF-β/Smad3 signaling pathway in an Nrf2-dependent manner. Free Radic Biol Med. 2018 Dec;129:446-453. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8725 mL | 19.3626 mL | 38.7252 mL | 96.8129 mL |
| 5 mM | 0.7745 mL | 3.8725 mL | 7.7450 mL | 19.3626 mL | |
| 10 mM | 0.3873 mL | 1.9363 mL | 3.8725 mL | 9.6813 mL | |
| 15 mM | 0.2582 mL | 1.2908 mL | 2.5817 mL | 6.4542 mL | |
| 20 mM | 0.1936 mL | 0.9681 mL | 1.9363 mL | 4.8406 mL | |
| 25 mM | 0.1549 mL | 0.7745 mL | 1.5490 mL | 3.8725 mL | |
| 30 mM | 0.1291 mL | 0.6454 mL | 1.2908 mL | 3.2271 mL | |
| 40 mM | 0.0968 mL | 0.4841 mL | 0.9681 mL | 2.4203 mL | |
| 50 mM | 0.0775 mL | 0.3873 mL | 0.7745 mL | 1.9363 mL | |
| 60 mM | 0.0645 mL | 0.3227 mL | 0.6454 mL | 1.6135 mL | |
| 80 mM | 0.0484 mL | 0.2420 mL | 0.4841 mL | 1.2102 mL | |
| 100 mM | 0.0387 mL | 0.1936 mL | 0.3873 mL | 0.9681 mL |