MCT1 INHIBITOR III (C15-1305-350)

General description

A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC₅₀ = 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t_1/2 = 3.03 h, T_max = 0.667 h & C_max = 17.5 mg/L; 100 mg/kg, i.p.: t_1/2 = 3.19 h, T_max = 0.5 h & C_max = 61.333 mg/L).

A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC₅₀ = 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t_1/2 = 3.03 h, T_max = 0.667 h & C_max = 17.5 mg/L; 100 mg/kg, i.p.: t_1/2 = 3.19 h, T_max = 0.5 h & C_max = 61.333 mg/L).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MCT1

Reversible: yes

Target IC₅₀: 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Gurrapu, S., et al. 2015. ACS Med. Chem. Lett.6, 558.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 392.38. Empirical Formula: C₂₃H₁₇N₂NaO₃. Assay: ≥. 97% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. color: yellow. solubility: DMSO: 50 . mg/mL. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.