2445185-57-7
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
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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]. |
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| 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 |
| Molecular Formula | C26H20ClN3O6S |
|---|---|
| Molecular Weight | 537.97 |