Art. -Nr.: HY-19957

Zoligratinib

(Synonyms: Debio 1347; CH5183284)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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.

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Reinheit: 99.76%
CAS. Nr.: 1265229-25-1
Formel: C₂₀H₁₆N₆O
Molecular Weight:356.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Zoligratinib Chemical Structure

CAS. Nr.: 1265229-25-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	8.24 μM Compound: 5; debio-1347	Growth inhibition of mouse BaF3 cells harboring TEL-FGFR3 V555M mutant incubated for 72 hrs by Alamar blue assay Growth inhibition of mouse BaF3 cells harboring TEL-FGFR3 V555M mutant incubated for 72 hrs by Alamar blue assay	[PMID: 35436119]
CHO	IC₅₀	6.9 μM Compound: 8; CH5183284; Debio 1347	Inhibition of human ERG expressed in CHO cells assessed as reduction in channel currents at -80 mV holding potential by automated whole-cell patch clamp method Inhibition of human ERG expressed in CHO cells assessed as reduction in channel currents at -80 mV holding potential by automated whole-cell patch clamp method	[PMID: 27933954]
HCT-116	IC₅₀	5900 nM Compound: 8; CH5183284; Debio 1347	Antiproliferative activity against human HCT116 cells incubated for 4 days by CCK8 assay Antiproliferative activity against human HCT116 cells incubated for 4 days by CCK8 assay	[PMID: 27933954]
SNU-16	IC₅₀	17 nM Compound: 8; CH5183284; Debio 1347	Antiproliferative activity against human SNU16 cells incubated for 4 days by CCK8 assay Antiproliferative activity against human SNU16 cells incubated for 4 days by CCK8 assay	[PMID: 27933954]

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].

MedChemExpress (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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1265229-25-1
Appearance Solid
Molecular Weight 356.38
Formel C₂₀H₁₆N₆O
Color Off-white to yellow
SMILES

O=C(C1=C(N)N(C2=CC=C3N=C(C)NC3=C2)N=C1)C(N4)=CC5=C4C=CC=C5
Synonyms

Debio 1347; CH5183284
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Nature

Truncated FGFR2 is a clinically actionable oncogene in multiple cancers. [Abstract]

2022 Aug;608(7923):609-617. PMID: 35948633
Cell Rep

IMPDH2 dephosphorylation under FGFR signaling promotes S-phase progression and tumor growth. [Abstract]

2024 Dec 30;44(1):115116. PMID: 39739531
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (70.15 mM; ultrasonic and warming and heat to 50°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Nakanishi Y, et al. The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014 Nov;13(11):2547-58. [Content Brief]

[2]. Nakanishi Y, et al. Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1. Mol Cancer Ther. 2015 Mar;14(3):704-12. [Content Brief]

[3]. Nakanishi Y, et al. ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor. Mol Cancer Ther. 2015 Dec;14(12):2831-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8060 mL	14.0300 mL	28.0599 mL	70.1498 mL
	5 mM	0.5612 mL	2.8060 mL	5.6120 mL	14.0300 mL
	10 mM	0.2806 mL	1.4030 mL	2.8060 mL	7.0150 mL
	15 mM	0.1871 mL	0.9353 mL	1.8707 mL	4.6767 mL
	20 mM	0.1403 mL	0.7015 mL	1.4030 mL	3.5075 mL
	25 mM	0.1122 mL	0.5612 mL	1.1224 mL	2.8060 mL
	30 mM	0.0935 mL	0.4677 mL	0.9353 mL	2.3383 mL
	40 mM	0.0701 mL	0.3507 mL	0.7015 mL	1.7537 mL
	50 mM	0.0561 mL	0.2806 mL	0.5612 mL	1.4030 mL
	60 mM	0.0468 mL	0.2338 mL	0.4677 mL	1.1692 mL

Keywords

Zoligratinib

3 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Zoligratinib

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zoligratinib Related Classifications

HY-19957 Related Classifications