A potent inhibitor of JAK1 and JAK2
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CYT387

Item No. 16246

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide
CAS Number
1056634-68-4
Synonyms
  • Momelotinib
Molecular Formula
C23H22N6O2
Formula Weight
414.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMSO: 16 mg/ml
λmax
292 nm
SMILES
O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2
InChi Code
InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)
InChi Key
ZVHNDZWQTBEVRY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $90

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    5 mg

    $132

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    10 mg

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    50 mg

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    Product Description

    CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively).1,2 It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM).1 At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines.1 It is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms, although kinase domain mutations can confer resistance.1,3 CYT387 also blocks paclitaxel-induced JAK2 activation in ovarian cancer cells, preventing the development of a cancer stem cell-like population following chemotherapy.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tyner, J.W., Bumm, T.G., Deininger, J., et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 115(25), 5232-5240 (2010).

    2. Furqan, M., Mukhi, N., Lee, B., et al. Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical application. Biomark. Res. 1(1), 5 (2013).

    3. Deshpande, A., Reddy, M.M., Schade, G.O.M., et al. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26(4), 708-715 (2012).

    4. Abubaker, K., Luwor, R.B., Zhu, H., et al. Inhibition of the JAK2/STAT3 pathway in ovarian cancer results in the loss of cancer stem cell-like characteristics and a reduced tumor burden. BMC Cancer 14, 317 (2014).