1. Immunology/Inflammation
    Metabolic Enzyme/Protease
  2. COX
    Carbonic Anhydrase
  3. Polmacoxib

Polmacoxib (Synonyms: CG100649)

Cat. No.: HY-16726 Purity: 99.70%
Handling Instructions

Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models.

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

Polmacoxib Chemical Structure

Polmacoxib Chemical Structure

CAS No. : 301692-76-2

Size Price Stock Quantity
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 680 In-stock
Estimated Time of Arrival: December 31
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Description

Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2].

IC50 & Target[1]

COX-2

0.1 μg/mL (IC50)

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 ApcMin/+ 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.

Molecular Weight

361.39

Formula

C18H16FNO4S

CAS No.
SMILES

O=S(C1=CC=C(C(OC2(C)C)=C(C3=CC=CC(F)=C3)C2=O)C=C1)(N)=O

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
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Product Name:
Polmacoxib
Cat. No.:
HY-16726
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