LY3200882
Based on 14 publication(s) in Google Scholar
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.87%
- CAS No.: 1898283-02-7
- Formule: C24H29N5O3
- Masse moléculaire:435.52
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LY3200882
More- Nat Genet. 2025 Dec;57(12):3050-3065. [Abstract]
- Sci Adv. 2022 Nov 25;8(47):eabo4116. [Abstract]
- Biomaterials. 2022 May;284:121518. [Abstract]
- J Invest Dermatol. 2025 Jan;145(1):65-76.e13. [Abstract]
- J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
- Mar Drugs. 2021 Sep 22;19(10):529. [Abstract]
- Bioengineering (Basel). 2024 Nov 20;11(11):1167. [Abstract]
- FASEB J. 2020 Aug;34(8):11168-11184. [Abstract]
- Cytokine. 2023 Apr:164:156139. [Abstract]
- Biol Reprod. 2024 Dec 12;111(6):1235-1248. [Abstract]
- Res Sq. 2025 Dec 10.
- Res Sq. 2025 Sep 26.
- Patent. US20240238274A1.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Apoptosis Analysis
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Cell Migration/Invasion Assay
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WB
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Histological Imaging/Staining
Activité biologique
Description
IC50 & Target
IC50: 38.2 nM (TGF-β receptor type 1 (ALK5))[2]
In Vitro
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells in a dose dependent fashion[1].
LY3200882 shows potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment[1].
In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation[1].
LY3200882 inhibits NIH3T3 cell viability with an IC50 of 82.9 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion[1].
LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C female mice (5-8-week-old) injected with CT26 cells[2]
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Dosage:60 mg/kg
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Administration:Oral gavage; twice a day; for 21 days
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Result:A statistically significant tumor growth delay in CT26 model was observed.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1898283-02-7
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Appearance Solid
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Masse moléculaire 435.52
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Formule C24H29N5O3
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Color Off-white to light yellow
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SMILES
OC(C)(C)C1=NC=CC(NC2=NC=CC(OC3=CN(C4CC4)N=C3C5CCOCC5)=C2)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Genet
TGF-β builds a dual immune barrier in colorectal cancer by impairing T cell recruitment and instructing immunosuppressive SPP1+ macrophages. [Abstract]2025 Dec;57(12):3050-3065. PMID: 41203813 -
Sci Adv
2022 Nov 25;8(47):eabo4116. PMID: 36427305 -
Biomaterials
The programmed site-specific delivery of LY3200882 and PD-L1 siRNA boosts immunotherapy for triple-negative breast cancer by remodeling tumor microenvironment. [Abstract]2022 May;284:121518. PMID: 35462305 -
J Invest Dermatol
Identification of Small-Molecule Inhibitors Targeting Different Signaling Pathways in Cancer-Associated Fibroblast Reprogramming Under Tumor-Stroma Interaction. [Abstract]2025 Jan;145(1):65-76.e13. PMID: 38848988 -
J Biol Eng
Enhancing the therapeutic efficacy of gemcitabine in bladder cancer through TGF-β1 inhibition and pluronic F-127-based microsphere delivery. [Abstract]2025 Jul 11;19(1):62. PMID: 40646590
LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
Bladder cancer cell lines 5637 and SW780 were treated with varying concentrations of LY3200882 (0, 1, 2.5, or 5 µM) for 48 h and assessed for cell viability using CCK8 assay.
LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
Cells were treated with 2.5 µM LY2109761 or LY3200882 and examined for cell apoptosis by Flow cytometry.
LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
Cell invasion capabilities using a Transwell assay treated with 2.5 µM LY2109761 or LY3200882.
LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
The protein levels of Ki-67, Cleaved-caspase 3, E-cadherin, MMP-2, and MMP-9 using Immunoblotting treated with 2.5 µM LY2109761 or LY3200882.
LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
Histological analysis of tumor tissues treated with LY3200882 (10 mg/kg) using H&E staining.
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Mar Drugs
Anti-Inflammatory Azaphilones from the Edible Alga-Derived Fungus Penicillium sclerotiorum. [Abstract]2021 Sep 22;19(10):529. PMID: 34677428 -
Bioengineering (Basel)
2024 Nov 20;11(11):1167. PMID: 39593826 -
FASEB J
Myeloid-specific blockade of Notch signaling alleviates murine pulmonary fibrosis through regulating monocyte-derived Ly6clo MHCIIhi alveolar macrophages recruitment and TGF-β secretion. [Abstract]2020 Aug;34(8):11168-11184. PMID: 32638441 -
Cytokine
Bone marrow mesenchymal stem cells paracrine TGF-β1 to mediate the biological activity of osteoblasts in bone repair. [Abstract]2023 Apr:164:156139. PMID: 36738525 -
Biol Reprod
2024 Dec 12;111(6):1235-1248. PMID: 39012723 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
Solvant et solubilité
In Vitro:
DMSO : 33.33 mg/mL (76.53 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (5.74 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.74 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2961 mL | 11.4805 mL | 22.9611 mL | 57.4026 mL |
| 5 mM | 0.4592 mL | 2.2961 mL | 4.5922 mL | 11.4805 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2961 mL | 5.7403 mL | |
| 15 mM | 0.1531 mL | 0.7654 mL | 1.5307 mL | 3.8268 mL | |
| 20 mM | 0.1148 mL | 0.5740 mL | 1.1481 mL | 2.8701 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9184 mL | 2.2961 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9134 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4351 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1481 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3827 mL | 0.9567 mL |
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