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

Roblitinib  (Synonyms: FGF-401)

Cat. No.: HY-101568 Purity: 99.74%
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Roblitinib (FGF-401; Compound Example 83) est un inhibiteur de FGFR4 qui est hautement sélectif et puissant avec un IC50 de 1,9 nM. Roblitinib a une activité antitumorale.

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.

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

Roblitinib Chemical Structure

Roblitinib Chemical Structure

CAS No. : 1708971-55-4

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Based on 5 publication(s) in Google Scholar

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Description

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM[1]. Roblitinib has antitumor activity[2].

IC50 & Target[1][2]

FGFR4

1.9 nM (IC50)

FGFR1

>10 μM (IC50)

FGFR2

>10 μM (IC50)

FGFR3

>10 μM (IC50)

rat FGFR4

>10 μM (IC50)

In Vitro

Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC50= 1.9 nM)[1].
Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC50>10 uM)[1].
Roblitinib inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), HEPG2 (IC50>10 uM), JHH (IC50>10 uM)[1].

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

In Vivo

Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model[1].
Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days[1].
Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) [1].
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min•kg, and a Vss of 3.9 L/kg for male SD rats[1].

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

Animal Model: Male Wistar Hannover rats (Hep3B xenograft model)[1]
Dosage: 10, 30, 100 mg/kg
Administration: Gavage; for 10 days
Result: Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.
Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.
Animal Model: Male mice (C57BL/6)[1]
Dosage: 1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis)
Administration: IV at 1 mg/kg; PO at 3 mg/kg
Result: Had a T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg.
Clinical Trial
Molecular Weight

506.56

Formula

C25H30N8O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1CC(N(CC2=CC(CCCN3C(NC4=CC(NCCOC)=C(C#N)C=N4)=O)=C3N=C2C=O)CC1)=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 (9.87 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 1.9741 mL 9.8705 mL 19.7410 mL
5 mM 0.3948 mL 1.9741 mL 3.9482 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.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.74%

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 1.9741 mL 9.8705 mL 19.7410 mL 49.3525 mL
5 mM 0.3948 mL 1.9741 mL 3.9482 mL 9.8705 mL
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Roblitinib 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.

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Roblitinib
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