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

Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model.

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Irpagratinib

Irpagratinib 화학구조

CAS No. : 2230974-62-4

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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Irpagratinib Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model[1][2].

IC50 & Target

FGFR4[1]
In Vitro

Irpagratinib irreversibly modifies the Cys552 residue within the FGFR4 active site and is selective for FGFR4. Irpagratinib has shown potent antitumor activity in a hepatocellular carcinoma model[1].

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

Irpagratinib Related Antibodies
In Vivo

ABSK-011 (oral) dose-dependently inhibits the growth of subcutaneous xenograft tumors with FGFR4 activity and induced tumor regression. Safety studies shows that ABSK-011 had no inhibitory effect on CYP family members, hERG, etc[1].

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

570.59

화학식

C28H32F2N6O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(C(OC)=CC(OC)=C1F)=C1C2=CC(C=N3)=C(C(N4CC(C)(C4)OC)=N2)N=C3N[C@H]5[C@H](CCOC5)NC(C=C)=O
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : 100 mg/mL (175.26 mM; Need ultrasonic; 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 1.7526 mL 8.7629 mL 17.5257 mL
5 mM 0.3505 mL 1.7526 mL 3.5051 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.38 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (4.38 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7526 mL 8.7629 mL 17.5257 mL 43.8143 mL
5 mM 0.3505 mL 1.7526 mL 3.5051 mL 8.7629 mL
10 mM 0.1753 mL 0.8763 mL 1.7526 mL 4.3814 mL
15 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9210 mL
20 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
25 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7526 mL
30 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
40 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0954 mL
50 mM 0.0351 mL 0.1753 mL 0.3505 mL 0.8763 mL
60 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
80 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.5477 mL
100 mM 0.0175 mL 0.0876 mL 0.1753 mL 0.4381 mL
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Irpagratinib 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:

Irpagratinib2230974-62-4ABSK011ABSK 011ABSK-011FGFRFibroblast growth factor receptorantineoplasticanti-tumorauto-phosphorylationhigh exposureInhibitorinhibitorinhibit

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상품명:
Irpagratinib
Cat. No.:
HY-156618
수량:
MCE Japan Authorized Agent:

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