INCB053914

This product is for research use only, not for human use. We do not sell to patients.

INCB053914
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$1980To Be Confirmed
250mg$3200To Be Confirmed
500mg$4800To Be Confirmed

Cat #: V4089 CAS #: 1620012-39-6 Purity ≥ 98%

Description: INCB053914 is a novel, potent, selective, and ATP-competitive small molecule pan-inhibitor of PIM (Proviral Integration site of Moloney murine leukemia virus) kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.

References: 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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Molecular Weight (MW)513.52
Molecular FormulaC26H26F3N5O3
CAS No.1620012-39-6
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥ 10 mg/mLr
Water: N/Ar
Ethanol: N/A
SMILES CodeO=C(NC1=CN=C2C(CC[C@H]2O)=C1N3C[C@@H](N)[C@H](O)[C@@H](C)C3)C4=NC(C5=C(F)C=C C=C5F)=C(F)C=C4
SynonymsINCB53914; INCB-53914; INCB 53914; INCB053914; INCB-053914; INCB 053914
ProtocolIn VitroPIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib (mean IC50, 4 nM and 27 nM, respectively). Uzansertib (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. Uzansertib 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.
In VivoUzansertib 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). Uzansertib (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) .
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.9473 mL9.7367 mL19.4734 mL38.9469 mL
5mM0.3895 mL1.9473 mL3.8947 mL7.7894 mL
10mM0.1947 mL0.9737 mL1.9473 mL3.8947 mL
20mM0.0974 mL0.4868 mL0.9737 mL1.9473 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
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Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.