1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Pemigatinib

Pemigatinib (Synonyms: INCB054828)

Cat. No.: HY-109099 Purity: 98.95%
Handling Instructions

Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.

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

Pemigatinib Chemical Structure

Pemigatinib Chemical Structure

CAS No. : 1513857-77-6

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma[1][2].

IC50 & Target[2]

FGFR1

0.4 nM (IC50)

FGFR2

0.5 nM (IC50)

FGFR3

1.2 nM (IC50)

FGFR4

30 nM (IC50)

In Vitro

This hypothesis is corroborated with in vitro cell-based studies in which cells expressing FGFR2-CLIP1 fusion are sensitive to Pemigatinib (INCB054828; IC50 value of 10.16 nM), whereas cells with the addition of the N549H mutation are resistant to Pemigatinib (IC50 value of 1527.57 nM)[3].

Clinical Trial
Molecular Weight

487.50

Formula

C₂₄H₂₇F₂N₅O₄

CAS No.

1513857-77-6

SMILES

CCN(C(N(C(C(F)=C(OC)C=C1OC)=C1F)C2)=O)C(C2=CN3)=C4C3=NC(CN5CCOCC5)=C4

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 : 41.67 mg/mL (85.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0513 mL 10.2564 mL 20.5128 mL
5 mM 0.4103 mL 2.0513 mL 4.1026 mL
10 mM 0.2051 mL 1.0256 mL 2.0513 mL
*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: 2.08 mg/mL (4.27 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

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

Purity: 98.95%

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Keywords:

PemigatinibINCB054828INCB 054828INCB-054828FGFRFibroblast growth factor receptorOrallycholangiocarcinomaantineoplasticInhibitorinhibitorinhibit

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Pemigatinib
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HY-109099
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