1. JAK/STAT Signaling
  2. Pim
  3. INCB053914 phosphate

INCB053914 phosphate 

Cat. No.: HY-101870B Purity: 99.91%
Handling Instructions

INCB053914 phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. INCB053914 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.

For research use only. We do not sell to patients.

INCB053914 phosphate Chemical Structure

INCB053914 phosphate Chemical Structure

CAS No. : 2088852-47-3

Size Price Stock Quantity
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1560 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3480 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

INCB053914 phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. INCB053914 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines[1].

IC50 & Target[1]

PIM1

0.24 nM (IC50)

PIM2

30 nM (IC50)

PIM3

0.12 nM (IC50)

In Vitro

INCB053914 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[1].
INCB053914 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[1].
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by INCB053914 phosphate (mean IC50, 4 nM and 27 nM, respectively)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

INCB053914 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) [1].
INCB053914 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) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)[1]
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.
Clinical Trial
Molecular Weight

611.51

Formula

C₂₆H₂₉F₃N₅O₇P

CAS No.
SMILES

O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=CN=C4C(CC[[email protected]]4O)=C3N5C[[email protected]@H](N)[[email protected]](O)[[email protected]@H](C)C5.OP(O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (8.18 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6353 mL 8.1765 mL 16.3530 mL
5 mM 0.3271 mL 1.6353 mL 3.2706 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.91%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

INCB053914INCB 053914INCB-053914PimPim kinasesorallyATP-competitivebroadanti-proliferativeactivityhematologictumorcelllinesmalignanciesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
INCB053914 phosphate
Cat. No.:
HY-101870B
Quantity:
MCE Japan Authorized Agent: