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  • DC Chemicals Limited
  • China
  • Product Name: MCT4-IN-1
  • Price: ¥Inquiry/100mg ¥Inquiry/250mg ¥Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 1 Day
  • Contact: Tony Cao

2445185-57-7

2445185-57-7 structure
2445185-57-7 structure
  • Name: MCT4-IN-1
  • Chemical Name: MCT4-IN-1
  • CAS Number: 2445185-57-7
  • Molecular Formula: C26H20ClN3O6S
  • Molecular Weight: 537.97
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Monocarboxylate Transporter
  • Create Date: 2021-10-24 10:20:19
  • Modify Date: 2024-01-11 17:11:48
  • MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research[1].

Name MCT4-IN-1
Description MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research[1].
Related Catalog
In Vitro MCT4-IN-1 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC50 of 1 nM. The on-target activity is confirmed with a Ki of 11 nM by fluorescence cross-correlation spectroscopy (FCCS)[1]. MCT4-IN-1 does not inhibit lactate efflux to a similar extent in SNU-398 and MiaPaca2, and only 600-fold less in RT-4 cell lines[1].
In Vivo MCT4-IN-1 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation[1]. MCT4-IN-1 (30 mg/kg/day; for 15 days) shows no significant antitumor activity[1]. MCT4-IN-1 (0.2 mg/kg; iv) has a T1/2 of 1 hours, a CL of 0.33 L/h•kg, a Cmax of 489 ng/mL and a Vss of 0.4 L/kg for mice[1]. Animal Model: MC38 tumor-bearing C57/BL6 mice[1] Dosage: 30 mg/kg Administration: PO; single dose Result: Only combined with MCT1/2 inhibitor exhibited a significant tumoral intracellular lactate accumulation. Animal Model: Mice[1] Dosage: 0.2 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a T1/2 of 1 hours, a CL of 0.33 L/h•kg, a Cmax of 489 ng/mL and a Vss of 0.4 L/kg for mice.
References

[1]. Timo Heinrich, et al. Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology. J Med Chem. 2021 Aug 26;64(16):11904-11933.

Molecular Formula C26H20ClN3O6S
Molecular Weight 537.97