Art. -Nr.: HY-131908

CPL304110

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CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), with IC₅₀ values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.

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Reinheit: 99.85%
CAS. Nr.: 1627826-19-0
Formel: C₂₅H₃₀N₆O₂
Molecular Weight:446.54

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CPL304110 Chemical Structure

CAS. Nr.: 1627826-19-0

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

FGFR1

0.75 nM (IC₅₀)

FGFR2

0.5 nM (IC₅₀)

FGFR3

3.05 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
AN3-CA	IC₅₀	392.8 nM Compound: 56q; CPL30411	Antiproliferative activity against human AN3-CA cells assessed as inhibition of cell growth Antiproliferative activity against human AN3-CA cells assessed as inhibition of cell growth	[PMID: 33199155]
BaF3	IC₅₀	227 nM Compound: 56q; CPL30411	Antiproliferative activity against mouse BaF3 cells transfected with TEL and FGFR1 gene assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells transfected with TEL and FGFR1 gene assessed as inhibition of cell growth	[PMID: 33199155]
NCI-H1581	IC₅₀	79.08 nM Compound: 56q; CPL30411	Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth	[PMID: 33199155]
SNU-16	IC₅₀	85.64 nM Compound: 56q; CPL30411	Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay	[PMID: 33199155]
SW780	IC₅₀	2562 nM Compound: 56q; CPL30411	Antiproliferative activity against human SW780 cells assessed as inhibition of cell growth Antiproliferative activity against human SW780 cells assessed as inhibition of cell growth	[PMID: 33199155]

In Vitro

CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK)^[1].
CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC₅₀ of 85.64 nM^[1].
CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases^[1].

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

Western Blot Analysis^[1]

Cell Line:

SNU-16 cell lines.
Concentration:

0-0.6 μM.
Incubation Time:

1 h.
Result:

Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK)

In Vivo

CPL304110 (p.o., 40 mg/kg) exhibits a t_1/2 of 2 h and C_max of 3369 ng/mL in mice^[1].
CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day^[1].

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

Animal Model:

Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human)^[1].
Dosage:

20 mg/kg (X2).
Administration:

Orally, twice daily for 21 days.
Result:

After 6 hours of last dosing, concentration of 56q decreased in the plasma (9%) but increased stepwise in the tumor cells (121%).

Clinical Trial

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

Chemical Information

CAS. Nr. 1627826-19-0
Appearance Solid
Molecular Weight 446.54
Formel C₂₅H₃₀N₆O₂
Color White to light yellow
SMILES

CN(CC1)CCN1C2=CC3=C(N=C(C4=NNC(CCC5=CC(OC)=CC(OC)=C5)=C4)N3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (223.94 mM; Need ultrasonic; 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

2.2394 mL

11.1972 mL

22.3944 mL

5 mM

0.4479 mL

2.2394 mL

4.4789 mL

10 mM

0.2239 mL

1.1197 mL

2.2394 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, 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.

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: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Abdellah Yamani, et al. Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). Eur J Med Chem. 2020 Nov 7;112990. [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, 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	2.2394 mL	11.1972 mL	22.3944 mL	55.9860 mL
	5 mM	0.4479 mL	2.2394 mL	4.4789 mL	11.1972 mL
	10 mM	0.2239 mL	1.1197 mL	2.2394 mL	5.5986 mL
	15 mM	0.1493 mL	0.7465 mL	1.4930 mL	3.7324 mL
	20 mM	0.1120 mL	0.5599 mL	1.1197 mL	2.7993 mL
	25 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2394 mL
	30 mM	0.0746 mL	0.3732 mL	0.7465 mL	1.8662 mL
	40 mM	0.0560 mL	0.2799 mL	0.5599 mL	1.3997 mL
	50 mM	0.0448 mL	0.2239 mL	0.4479 mL	1.1197 mL
	60 mM	0.0373 mL	0.1866 mL	0.3732 mL	0.9331 mL
	80 mM	0.0280 mL	0.1400 mL	0.2799 mL	0.6998 mL
	100 mM	0.0224 mL	0.1120 mL	0.2239 mL	0.5599 mL

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CPL304110

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CPL304110

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CPL304110 Related Classifications

HY-131908 Related Classifications