Art. -Nr.: HY-120797

CRT0273750

(Synonyms: IOA-289)

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CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC₅₀ = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.

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Reinheit: 98.87%
CAS. Nr.: 1979939-16-6
Formel: C₂₅H₂₂ClF₃N₄O₂
Molecular Weight:502.92

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CRT0273750 Chemical Structure

CAS. Nr.: 1979939-16-6

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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

CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC₅₀ = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer^[1].

IC₅₀ & Target

IC50: 0.014 μM (plasma CRA)

Alle LPL Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	EC₅₀	0.025 μM Compound: 9v; CRT0273750	Inhibition of human recombinant ATX/LPC 18:1-mediated mouse 4T1 cell migration after overnight incubation by Transwell assay Inhibition of human recombinant ATX/LPC 18:1-mediated mouse 4T1 cell migration after overnight incubation by Transwell assay	[PMID: 27780639]

In Vitro

CRT0273750 shows high potency in both the biochemical (IC₅₀ = 0.01 μM) and plasma choline release assay(IC₅₀ = 0.014 μM)^[1].
CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM^[1].

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

In Vivo

CRT0273750 (1 mg/kg; i.v.)has a moderate blood clearance, with value of 41 mL/min/kg^[1].
CRT0273750 (10 mg/kg; oral administration) treatment shows the C_max, AUC and t_1/2 values of 3.8 μM, 3.2 μM.h and 1.4 h, respectively^[1].

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

Animal Model:

CD-1 mice^[1]
Dosage:

1 mg/kg
Administration:

I.v.
Result:

Had a moderate blood clearance.

Animal Model:

Balb-c nu/nu mice^[1]
Dosage:

10, 30 and 100 mg/kg
Administration:

Oral administration (Pharmacokinetic Analysis)
Result:

The C_maxs were 3.8, 10.9 and 18.1 µM, respectively.
The AUCs were 3.2, 15.2 and 59.3 µM.h, respectively.
The t_1/2s were 1.4, 0.9 and 1.3 h, respectively.

Clinical Trial

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

Chemical Information

CAS. Nr. 1979939-16-6
Appearance Solid
Molecular Weight 502.92
Formel C₂₅H₂₂ClF₃N₄O₂
Color White to off-white
SMILES

FC(F)(OC1=CC=C(C=C1)CN2C(CCC(N[C@H](C3=CC=C(Cl)C=C3)C)=O)=NC4=CC=CN=C42)F
Synonyms

IOA-289
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 175 mg/mL (347.97 mM; ultrasonic and warming and heat to 60°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

1.9884 mL

9.9419 mL

19.8839 mL

5 mM

0.3977 mL

1.9884 mL

3.9768 mL

10 mM

0.1988 mL

0.9942 mL

1.9884 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: ≥ 2.08 mg/mL (4.14 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.14 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Shah P, et al. Discovery of potent inhibitors of the lysophospholipase autotaxin. Bioorg Med Chem Lett. 2016;26(22):5403-5410. [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	1.9884 mL	9.9419 mL	19.8839 mL	49.7097 mL
	5 mM	0.3977 mL	1.9884 mL	3.9768 mL	9.9419 mL
	10 mM	0.1988 mL	0.9942 mL	1.9884 mL	4.9710 mL
	15 mM	0.1326 mL	0.6628 mL	1.3256 mL	3.3140 mL
	20 mM	0.0994 mL	0.4971 mL	0.9942 mL	2.4855 mL
	25 mM	0.0795 mL	0.3977 mL	0.7954 mL	1.9884 mL
	30 mM	0.0663 mL	0.3314 mL	0.6628 mL	1.6570 mL
	40 mM	0.0497 mL	0.2485 mL	0.4971 mL	1.2427 mL
	50 mM	0.0398 mL	0.1988 mL	0.3977 mL	0.9942 mL
	60 mM	0.0331 mL	0.1657 mL	0.3314 mL	0.8285 mL
	80 mM	0.0249 mL	0.1243 mL	0.2485 mL	0.6214 mL
	100 mM	0.0199 mL	0.0994 mL	0.1988 mL	0.4971 mL

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CRT0273750

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CRT0273750

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CRT0273750 Related Classifications

HY-120797 Related Classifications