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

Pemigatinib  (Synonyms: INCB054828)

Cat. No.: HY-109099 Purity: 99.73%
COA Handling Instructions

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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

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 129 In-stock
Solution
10 mM * 1 mL in DMSO USD 129 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 350 In-stock
50 mg USD 550 In-stock
100 mg USD 950 In-stock
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Based on 10 publication(s) in Google Scholar

Pemigatinib Related Antibodies

Top Publications Citing Use of Products

View All FGFR Isoform Specific Products:

View All Isoforms
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

Cells expressing the FGFR2-CLIP1 fusion is sensitive to Pemigatinib (INCB054828; IC50 value 10.16 nM), while cells with added N549H mutation is resistant to Pemigatinib (IC50 value of 1527.57 nM)[3].

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

Pemigatinib Related Antibodies
Clinical Trial
Molecular Weight

487.50

Formula

C24H27F2N5O4
CAS No.
Appearance

Solid

Color

White to light yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (51.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (5.64 mM); Clear solution

  • Protocol 2

    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

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.73%

COA (251 KB) HNMR (192 KB) LCMS (111 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0513 mL 10.2564 mL 20.5128 mL 51.2821 mL
5 mM 0.4103 mL 2.0513 mL 4.1026 mL 10.2564 mL
10 mM 0.2051 mL 1.0256 mL 2.0513 mL 5.1282 mL
15 mM 0.1368 mL 0.6838 mL 1.3675 mL 3.4188 mL
20 mM 0.1026 mL 0.5128 mL 1.0256 mL 2.5641 mL
25 mM 0.0821 mL 0.4103 mL 0.8205 mL 2.0513 mL
30 mM 0.0684 mL 0.3419 mL 0.6838 mL 1.7094 mL
40 mM 0.0513 mL 0.2564 mL 0.5128 mL 1.2821 mL
50 mM 0.0410 mL 0.2051 mL 0.4103 mL 1.0256 mL
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Pemigatinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pemigatinib1513857-77-6INCB054828INCB 054828INCB-054828FGFRFibroblast growth factor receptorOrallycholangiocarcinomaantineoplasticInhibitorinhibitorinhibit

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