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

Zoligratinib  (Synonyms: Debio 1347; CH5183284)

Cat. No.: HY-19957 Purity: 99.76%
COA Handling Instructions

Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

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

Zoligratinib Chemical Structure

Zoligratinib Chemical Structure

CAS No. : 1265229-25-1

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Solution
10 mM * 1 mL in DMSO USD 67 In-stock
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10 mM * 1 mL
ready for reconstitution
 USD 67 In-stock
Solid
5 mg USD 61 In-stock
10 mg USD 99 In-stock
25 mg USD 165 In-stock
50 mg USD 275 In-stock
100 mg USD 495 In-stock
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Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

IC50 & Target[1]

FGFR1

9.3 nM (IC50)

FGFR2

7.6 nM (IC50)

FGFR3

22 nM (IC50)

FGFR4

290 nM (IC50)

In Vitro

Zoligratinib is well balanced in cellular antiproliferative activity against SNU-16 and stability in human liver microsome. The selectivity of 8 to inhibit FGFR over KDR is suggested to be caused by the difference in the interaction with M535 in FGFR1 and L889 in KDR[1]. The IC50 of Zoligratinib is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation[2].

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

Zoligratinib treatment shows a dose-dependent tumor regression (tumor growth inhibition (TGI)=106% at 30 mg/kg and 147% at 100 mg/kg) without apparent body weight loss. Zoligratinib treatment also shows significant in vivo efficacy in xenograft mice models with FGFR genetic alterations, such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), MFE280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion)[1].

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

356.38

Appearance

Solid

Formula

C20H16N6O
CAS No.
SMILES

O=C(C1=C(N)N(C2=CC=C3N=C(C)NC3=C2)N=C1)C(N4)=CC5=C4C=CC=C5
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 : 25 mg/mL (70.15 mM; ultrasonic and warming and heat to 50°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8060 mL 14.0300 mL 28.0599 mL
5 mM 0.5612 mL 2.8060 mL 5.6120 mL
10 mM 0.2806 mL 1.4030 mL 2.8060 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.76%

COA (251 KB) LCMS (256 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

The cell lines are added to the wells of 96-well plates containing 0.076−10,000 nM tested compounds (CH5183284) and incubated at 37°C. After 4 days’ incubation, Cell Counting Kit-8 solution is added, and after incubation for several more hours, absorbance at 450 nm is measured. The antiproliferative activity is calculated using the formula (1-T/C) × 100 (%), where T and C represent absorbance at 450 nm of the cells treated with drugs (T) and that of untreated control cells (C)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Rats: Male Wistar rats (340-390 g) implanted with a telemetry transmitter are used for the assessment of effects on blood pressure (BP). Vehicle (0.5% carmellose sodium, 0.5% polysorbate 20, and 0.9% benzyl alcohol in purified water) or CH5183284/Debio 1347 (10 and 30 mg/kg) are administered by oral gavage once a day for 4 consecutive days. Data for blood pressure are automatically analyzed and continuously recorded at 5-minute intervals[2].

Mice: The in vivo efficacy is evaluated in mice bearing an SNU-16 xenograft. CH5183284 is orally administered once daily for 11 days, and the body weight of mice and the volume of the tumors are measured twice a week[1].

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

Zoligratinib1265229-25-1Debio 1347 CH5183284Debio1347Debio-1347CH5183284CH 5183284CH-5183284FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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