[CAS NO. 301692-76-2] Polmacoxib

Name: Polmacoxib
Brand: Arctom Scientific
SKU: AS263941

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PRODUCTS SPECIFICATIONS [301692-76-2]

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Catalog

AS263941

Brand

Arctom Scientific

CAS

301692-76-2

DESCRIPTION [301692-76-2]

Overview

MDL	-
Molecular Weight	361.39
Molecular Formula	C18H16FNO4S
SMILES	O=S(C1=CC=C(C(OC2(C)C)=C(C3=CC=CC(F)=C3)C2=O)C=C1)(N)=O

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

Summary

Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC ₅₀ around 0.1 μg/ml) and carbonic anhydrase ^[1] . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models ^[2] .

IC50 & Target

COX-2

0.1 μg/mL (IC ₅₀ )

carbonic anhydrase

In Vitro

Polmacoxib (CG100649) (0-1 μg/ml; 24 hours; HCA-7 and HT-29 cells) can inhibit COX-2 activity and PGE2 production in human colon cancer cells, at lower concentrations compared to Celecoxib ^[2] .

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

In Vivo

Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in Apc ^Min/+ mice ^[2] .
Polmacoxib (7-15 mg/kg; p.o.; daily from day 27 post-injection to day 111; athymic nude mice; subcutaneous xenograft mouse model) reduces tumor volume and tumor weight by 58% and 48%, respectively, compared to a 48% and 36% reduction following treatment with Celecoxib ^[2] .
Polmacoxib (7-15 mg/kg; p.o.; began on day 14 and continued for 8 weeks; athymic nu/nu mice; orthotopic xenograft mouse model) inhibits CRC growth in an orthotopic xenograft mouse model, reducing tumor weight by 70% using 7 mg/kg or by 83% using 15 mg/kg, compared to a similar 70% reduction following treatment with 500 mg/kg of Celecoxib ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03775629	CrystalGenomics, Inc.	Healthy	December 1, 2018	Phase 1
NCT00530452	CrystalGenomics, Inc.\|Quintiles, Inc.	Osteoarthritis, Knee\|Osteoarthritis, Hip	October 2007	Phase 2
NCT01154764	CrystalGenomics, Inc.	Healthy	October 2009	Phase 1
NCT01765296	CrystalGenomics, Inc.	Localized Primary Osteoarthritis of Hip\|Localized Primary Osteoarthritis of Knee	March 2013	Phase 3
NCT01154790	CrystalGenomics, Inc.	Healthy	June 2010	Phase 1
NCT01341405	CrystalGenomics, Inc.	Osteoarthritis	April 2011	Phase 2
NCT05370716	CrystalGenomics, Inc.	Healthy	November 11, 2019	Phase 1
NCT00780325	University of Pennsylvania\|CrystalGenomics, Inc.	Healthy Volunteers	October 2008	Phase 1

Appearance

Solid

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 ( 691.77 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7671 mL	13.8355 mL	27.6709 mL
5 mM	0.5534 mL	2.7671 mL	5.5342 mL
10 mM	0.2767 mL	1.3835 mL	2.7671 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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

Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution

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

References

Synonyms

Benzenesulfonamide, 4-[3-(3-fluorophenyl)-4,5-dihydro-5,5-dimethyl-4-oxo-2-furanyl]-

4-[3-(3-Fluorophenyl)-4,5-dihydro-5,5-dimethyl-4-oxo-2-furanyl]benzenesulfonamide

CG 100649

Polmacoxib

Acelex