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CRT0273750 

Cat. No.: HY-120797
Handling Instructions

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.

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

CRT0273750 Chemical Structure

CRT0273750 Chemical Structure

CAS No. : 1979939-16-6

Size Price Stock Quantity
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
25 mg USD 540 In-stock
Estimated Time of Arrival: December 31
50 mg USD 920 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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)

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].

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 Cmax, AUC and t1/2 values of 3.8 µM, 3.2 µM.h and 1.4 h, respectively[1].
CRT0273750 (10, 30 and 100 mg/kg; oral administration) shows a proportional increase[1].

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 Cmaxs were 3.8, 10.9 and 18.1 µM, respectively.
The AUCs were 3.2, 15.2 and 59.3 µM.h, respectively.
The t1/2s were 1.4, 0.9 and 1.3 h, respectively.
Molecular Weight

502.92

Formula

C₂₅H₂₂ClF₃N₄O₂

CAS No.
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 : 250 mg/mL (497.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
CRT0273750
Cat. No.:
HY-120797
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