Art. -Nr.: HY-15270

BMS-911543

4 Cited Publications

Kundenbewertung

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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.23%
CAS. Nr.: 1271022-90-2
Formel: C₂₃H₂₈N₈O
Molecular Weight:432.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BMS-911543 Chemical Structure

CAS. Nr.: 1271022-90-2

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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).

IC₅₀ & Target^[1]

JAK2

1.1 nM (IC₅₀)

Tyk2

66 nM (IC₅₀)

JAK1

75 nM (IC₅₀)

JAK3

360 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2400 nM Compound: 11, BMS-911543	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	[PMID: 26288683]
BaF3	IC₅₀	3500 nM Compound: 11, BMS-911543	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	[PMID: 26288683]
BaF3	IC₅₀	65 nM Compound: 11, BMS-911543	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	[PMID: 26288683]
BaF3	IC₅₀	70 nM Compound: 11, BMS-911543	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	[PMID: 26288683]
HepG2	IC₅₀	>50 μM Compound: 11, BMS-911543	Toxicity against human HepG2 cells Toxicity against human HepG2 cells	[PMID: 26288683]
SET-2	IC₅₀	60 nM Compound: 11, BMS-911543	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	[PMID: 26288683]
T-cell	IC₅₀	990 nM Compound: 11, BMS-911543	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	[PMID: 26288683]

In Vitro

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.

In Vivo

BMS-911543 is well tolerated up to 100 mg/kg in rats (mean AUC_{0-72 h}, 11300 μM·h) and dogs (AUC_{0-24 h}, 610 μM·h). A 15 mg/kg/day dose (Day 14 AUC_{0-24 h}, 3200 μM·h) is well tolerated^[1] in two-week repeat dose studies in rats. BMS-911543 (30 mg/kg, p.o.) suppresses the growth of tumor and prolongs the median survival in KPC-Brca1 mice. BMS-911543 also selectively reduces pSTAT5 expression in pancreatic tumors and decreases levels of intratumoral FoxP3⁺ T regulatory cells in mice administered BMS-911543^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1271022-90-2
Appearance Solid
Molecular Weight 432.52
Formel C₂₃H₂₈N₈O
Color White to light yellow
SMILES

O=C(C1=CC2=C(N(C)C=N3)C3=C(NC4=NN(C)C(C)=C4)N=C2N1CC)N(C5CC5)C6CC6
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

All Cell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

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.
bioRxiv

2025 Oct 10.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3120 mL

11.5602 mL

23.1203 mL

5 mM

0.4624 mL

2.3120 mL

4.6241 mL

10 mM

0.2312 mL

1.1560 mL

2.3120 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[2]

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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

BMS-911543

4 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

BMS-911543

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) BMS-911543

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-911543 Related Classifications

HY-15270 Related Classifications