A potent, selective JAK2 inhibitor
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BMS-911543

Item No. 21088

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N-dicyclopropyl-4-[(1,5-dimethyl-1H-pyrazol-3-yl)amino]-6-ethyl-1,6-dihydro-1-methyl-imidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide
CAS Number
1271022-90-2
Molecular Formula
C23H28N8O
Formula Weight
432.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): slightly
λmax
227, 280, 342 nm
SMILES
CN1C=NC2=C1C(C=C(C(N(C3CC3)C4CC4)=O)N5CC)=C5N=C2NC6=NN(C)C(C)=C6
InChi Code
InChI=1S/C23H28N8O/c1-5-30-17(23(32)31(14-6-7-14)15-8-9-15)11-16-20-19(24-12-28(20)3)21(26-22(16)30)25-18-10-13(2)29(4)27-18/h10-12,14-15H,5-9H2,1-4H3,(H,25,26,27)
InChi Key
JCINBYQJBYJGDM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $297

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    10 mg

    $525

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    25 mg

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    Product Description

    BMS-911543 is a potent, selective ATP-competitive inhibitor of Janus kinase 2 (JAK2) that exhibits IC50 values of 1, 356, 73, and 66 nM for JAK2, JAK1, JAK3, and TYK2, respectively.1 It exhibits antiproliferative activity in a variety of cell lines engineered to express the JAK2V617F activating mutation (IC50s = 60-70 nM).1,2 BMS-911543 exhibited limited activity in a mouse model of JAK2V617F-driven myeloproliferative neoplasm.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Purandare, A.V., McDevitt, T.M., Wan, H.Y., D., et al. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia 26(2), 280-288 (2012).

    2. Wan, H., Schroeder, G.M., Hart, A.C., et al. Discovery of a highly selective JAK2 inhibitor, BMS-911543, for the treatment of myeloproliferative neoplasms. ACS Med. Chem. Lett. 6(8), 850-855 (2015).

    3. Pomicter, A.D., Eiring, A.M., Senina, A.V., et al. Limited efficacy of BMS-911543 in a murine model of Janus kinase 2 V617F myeloproliferative neoplasm. Exp. Hematol. 43(7), 537-545 (2015).