You are here:Home-Chemical Inhibitors & Agonists-JAK/STAT Signaling-Pim-INCB053914 phosphate
INCB053914 phosphate

Chemical Structure : INCB053914 phosphate

CAS No.: 2088852-47-3

INCB053914 phosphate

Catalog No.: PC-22079Not For Human Use, Lab Use Only.

INCB053914 (Uzansertib) phosphate is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.

Packing Price Stock Quantity
5 mg $288 In stock
10 mg $478 In stock
25 mg $798 In stock
50 mg Get quote
100 mg Get quote

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

INCB053914 (Uzansertib) phosphate is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.
INCB053914 is highly selective against a panel of more than 50 kinases (>475-fold selectivity) with exception of RSK2 (IC50=7.1 uM).
INCB053914 inhibits cellular proliferation in a panel of cell lines derived from hematologic malignancies including AML, MM, DLBCL, MCL, and T-ALL with GI50 of <100 nM, inhibits proliferation in all MM cell lines with GI5050 of 13.2-230.0 nM.
INCB053914 inhibits PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells with IC50 of 4 and 27 nM, also increases PIM2 expression in KG-1a (AML), Pfeiffer, and KMS12-PE cells.
INCB053914 inhibits Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.

Physicochemical Properties

M.Wt 611.51
Formula C26H29F3N5O7P
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Pyridinecarboxamide, N-[(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methyl-1-piperidinyl]-6,7-dihydro-7-hydroxy-5H-cyclopenta[b]pyridin-3-yl]-6-(2,6-difluorophenyl)-5-fluoro-, phosphate (1:1)

References

1. Koblish H, et al. PLoS One. 2018 Jun 21;13(6):e0199108.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: