1. Protein Tyrosine Kinase/RTK
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  3. Roblitinib

Roblitinib (Synonyms: FGF-401)

Cat. No.: HY-101568 Purity: 99.33%
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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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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].

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].

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.
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 : 5.2 mg/mL (10.27 mM; Need ultrasonic)

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
10 mM 0.1974 mL 0.9870 mL 1.9741 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.33%

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