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  3. Futibatinib

Futibatinib (Synonyms: TAS-120)

Cat. No.: HY-100818 Purity: 98.80%
Handling Instructions

Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).

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

Futibatinib Chemical Structure

Futibatinib Chemical Structure

CAS No. : 1448169-71-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 387 In-stock
Estimated Time of Arrival: December 31
1 mg USD 168 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Description

Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM)[1][2][3].

IC50 & Target[3]

FGFR1

3.9 nM (IC50)

FGFR2

1.3 nM (IC50)

FGFR3

1.6 nM (IC50)

FGFR4

8.3 nM (IC50)

wild-type FGFR2

0.3 nM (IC50)

FGFR2 V5651

1-3 nM (IC50)

FGFR2 N550H

3.6 nM (IC50)

FGFR2 E566G

2.4 nM (IC50)

In Vitro

Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR[1].

In Vivo

Futibatinib (TAS-120) (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. Futibatinib (TAS-120) shows anti-tumor effect by administering at moderate intervals, such as intermittent administration of every other day dosing and 2 times/week, and reducing the sustained elevation and weight suppression blood phosphorus level, and take a antitumor effective as daily administration[1].

Clinical Trial
Molecular Weight

418.45

Formula

C₂₂H₂₂N₆O₃

CAS No.

1448169-71-8

SMILES

O=C(C=C)N(C1)CC[[email protected]@H]1N(N=C2C#CC3=CC(OC)=CC(OC)=C3)C4=C2C(N)=NC=N4

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 : ≥ 29 mg/mL (69.30 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3898 mL 11.9489 mL 23.8977 mL
5 mM 0.4780 mL 2.3898 mL 4.7795 mL
10 mM 0.2390 mL 1.1949 mL 2.3898 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: ≥ 2.5 mg/mL (5.97 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution

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

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

Animal Administration
[1]

It is transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the old 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring the major axis of tumor (mm) and minor axis (mm) after tumor implantation, the tumor volume: After calculating the (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the days that are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, is prepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administered orally, 30 mg/kg/day is administered orally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, provided with the evaluation period of 14 days, the final valuation date it is day 15.

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

References

Purity: 98.80%

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Keywords:

FutibatinibTAS-120TAS120TAS 120FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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