INCB053914 phosphate

CAS No. 2088852-47-3

INCB053914 phosphate( —— )

Catalog No. M23938 CAS No. 2088852-47-3

INCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    INCB053914 phosphate
  • Note
    Research use only, not for human use.
  • Brief Description
    INCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase.
  • Description
    INCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively).(In Vitro):Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI50 values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines.Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines.PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC50, 4 nM and 27 nM, respectively).(In Vivo):Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) .Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC50=70 nM; KMS-12-BM tumors, IC50=145 nM) .
  • In Vitro
    Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI50 values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines. Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines. PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC50, 4 nM and 27 nM, respectively).
  • In Vivo
    Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) . Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC50=70 nM; KMS-12-BM tumors, IC50=145 nM) . Animal Model:Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)Dosage:25, 50, 75, 100 mg/kg Administration:PO; twice a day; for 15 days Result:Inhibited tumor growth in a dose-dependent manner in mice.
  • Synonyms
    ——
  • Pathway
    JAK/STAT Signaling
  • Target
    Pim
  • Recptor
    PIM1|PIM2|PIM3
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2088852-47-3
  • Formula Weight
    611.51
  • Molecular Formula
    C26H29F3N5O7P
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 5 mg/mL (8.18 mM; Need ultrasonic and warming)
  • SMILES
    O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=CN=C4C(CC[C@H]4O)=C3N5C[C@@H](N)[C@H](O)[C@@H](C)C5.O=P(O)(O)O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Koblish H, et al. Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies. PLoS One. 2018 Jun 21;13(6):e0199108.
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