BMS-911543
Based on 4 publication(s) in Google Scholar
BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).
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- Pureza: 98.23%
- No. CAS: 1271022-90-2
- Fòrmula: C23H28N8O
- Peso molecular:432.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) BMS-911543
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Cell Proliferation/Viability Assay
Actividad biológica
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JAK2 1.1 nM (IC50) |
Tyk2 66 nM (IC50) |
JAK1 75 nM (IC50) |
JAK3 360 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2400 nM
Compound: 11, BMS-911543
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Antiproliferative activity against human A549 cells incubated for 72 hrs by [3H] thymidine incorporation assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by [3H] thymidine incorporation assay
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[PMID: 26288683] |
| BaF3 | IC50 |
3500 nM
Compound: 11, BMS-911543
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Antiproliferative activity against IL3-stimulated mouse BAF3 cells incubated for 72 hrs by [3H] thymidine incorporation assay
Antiproliferative activity against IL3-stimulated mouse BAF3 cells incubated for 72 hrs by [3H] thymidine incorporation assay
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[PMID: 26288683] |
| BaF3 | IC50 |
65 nM
Compound: 11, BMS-911543
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Inhibition of JAK2 in mouse BAF3 cells assessed as reduction in STAT5 phosphorylation incubated for 2 hrs by Western blot method
Inhibition of JAK2 in mouse BAF3 cells assessed as reduction in STAT5 phosphorylation incubated for 2 hrs by Western blot method
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[PMID: 26288683] |
| BaF3 | IC50 |
70 nM
Compound: 11, BMS-911543
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Antiproliferative activity against mouse BAF3 cells expressing JAK2 V617F mutant incubated for 72 hrs by [3H] thymidine incorporation assay
Antiproliferative activity against mouse BAF3 cells expressing JAK2 V617F mutant incubated for 72 hrs by [3H] thymidine incorporation assay
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[PMID: 26288683] |
| HepG2 | IC50 |
>50 μM
Compound: 11, BMS-911543
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Toxicity against human HepG2 cells
Toxicity against human HepG2 cells
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[PMID: 26288683] |
| SET-2 | IC50 |
60 nM
Compound: 11, BMS-911543
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Antiproliferative activity against human SET2 cells incubated for 72 hrs by [3H] thymidine incorporation assay
Antiproliferative activity against human SET2 cells incubated for 72 hrs by [3H] thymidine incorporation assay
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[PMID: 26288683] |
| T-cell | IC50 |
990 nM
Compound: 11, BMS-911543
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Inhibition of JAK1/JAK3 in T cells (unknown origin) assessed as reduction in IL2-mediated cell proliferation
Inhibition of JAK1/JAK3 in T cells (unknown origin) assessed as reduction in IL2-mediated cell proliferation
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[PMID: 26288683] |
BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively). BMS-911543 displays IC50 of >25 μM for all targets except PDE4 (IC50, 5.6 μM). BMS-911543 exhibits potent antiproliferative effect on the SET-2 and BaF3-V617F engineered cell lines (both dependent upon JAK2 pathway), with IC50s of 60 and 70 nM, respectively, and such an effect on SET-2 and BaF3-V617F cells is correlated with similar activity on constitutively active pSTAT5 (IC50, 80 and 65 nM, respectively)[1]. BMS-911543 (>20 μM) is cytotoxic to murine or human pancreatic ductal adenocarcinoma (PDAC) cell lines. BMS-911543 (5 and 10 μM) also blocks T regulatory cell differentiation in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 1271022-90-2
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Appearance Solid
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Peso molecular 432.52
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Fòrmula C23H28N8O
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Color White to light yellow
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SMILES
O=C(C1=CC2=C(N(C)C=N3)C3=C(NC4=NN(C)C(C)=C4)N=C2N1CC)N(C5CC5)C6CC6
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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 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
IUBMB Life
MicroRNA-204 deregulation in lung adenocarcinoma controls the biological behaviors of endothelial cells potentially by modulating Janus kinase 2-signal transducer and activator of transcription 3 pathway. [Abstract]2018 Jan;70(1):81-91. PMID: 29281186
BMS-911543 purchased from MedChemExpress. Usage Cited in: IUBMB Life. 2018 Jan;70(1):81-91. [Abstract]
A549 cells are treated with TG101348 (3 nM), BMS-911543 (1.5 nM), and Stattic (2.5 lM) for 24 h, and the conditioned media are collected and applied for tube formation assay in HUVECs.
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Solvente y solubilidad
DMSO : 25 mg/mL (57.80 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)
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 (5.78 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.
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
Human and murine pancreatic ductal adenocarcinoma (PDAC) tumor cells or PSC are cultured in 96 well plates and the following day treated with BMS-911543 or DMSO vehicle control for 48 hours. After 48 hours, MTT reagent (ATCC) is added for 2 hours at 37°C. Samples are analyzed on a plate reader testing for absorbance at 450 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Pancreatic tumors are confirmed in KPC-Brca1 mice by bioluminescent imaging (BLI) at 5-6 weeks of age. Briefly, mice are maintained on isofluorane anesthesia and imaged 10-15 minutes following intraperitoneal injection of Luciferin on a heated platform. Animals with a pancreatic mass of approximately 50-100 mm3 are randomized, and treatment is initiated the day following imaging. Mice are then treated for 2 weeks by daily oral gavage at a dose of 30 mg/kg BMS-911543. Following 2 weeks of treatment, animals are euthanized via CO2 asphyxiation followed by cardiac puncture. Plasma, splenocytes and tumor tissue are collected for further analysis. Pathology is assessed by H&E to determine differentiation state of the tissue as PanIN, papillary carcincoma or PDAC. For long term in vivo experiments, 8 week old KPC-Brca1 mice with advanced disease are continuously treated by oral gavage at 30 mg/kg of BMS-911543 until mice meet specified early removal criteria[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 (281 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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wan H, et al. Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. [Content Brief]
[2]. Mace TA, et al. Single agent BMS-911543 Jak2 inhibitor has distinct inhibitory effects on STAT5 signaling in genetically engineered mice with pancreatic cancer. Oncotarget. 2015 Dec 29;6(42):44509-22. [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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3120 mL | 11.5602 mL | 23.1203 mL | 57.8008 mL |
| 5 mM | 0.4624 mL | 2.3120 mL | 4.6241 mL | 11.5602 mL | |
| 10 mM | 0.2312 mL | 1.1560 mL | 2.3120 mL | 5.7801 mL | |
| 15 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8534 mL | |
| 20 mM | 0.1156 mL | 0.5780 mL | 1.1560 mL | 2.8900 mL | |
| 25 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3120 mL | |
| 30 mM | 0.0771 mL | 0.3853 mL | 0.7707 mL | 1.9267 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4450 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL |
BMS-911543 Related Classifications
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