2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. BMS-911543

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).

For research use only. We do not sell to patients.

BMS-911543 Chemical Structure

BMS-911543 Chemical Structure

CAS No. : 1271022-90-2

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Customer Review

Based on 2 publication(s) in Google Scholar

BMS-911543 Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

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JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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]
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]
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.

BMS-911543 Related Antibodies
In Vivo

BMS-911543 is well tolerated up to 100 mg/kg in rats (mean AUC0-72 h, 11300 μM·h) and dogs (AUC0-24 h, 610 μM·h). A 15 mg/kg/day dose (Day 14 AUC0-24 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
Molecular Weight

432.52

Formula

C23H28N8O
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3120 mL 11.5602 mL 23.1203 mL
5 mM 0.4624 mL 2.3120 mL 4.6241 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.23%

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
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].

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].

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

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
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BMS-911543 Related Classifications

Keywords:

BMS-9115431271022-90-2BMS911543BMS 911543JAKJanus kinaseInhibitorinhibitorinhibit

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