909910-43-6
909910-43-6 structure
- Name: A 83-01
- Chemical Name: 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
- CAS Number: 909910-43-6
- Molecular Formula: C25H19N5S
- Molecular Weight: 421.51700
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK ALK
- Create Date: 2018-12-18 12:00:11
- Modify Date: 2024-01-12 19:15:50
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A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.
| Name | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide |
|---|---|
| Synonyms |
A-83-01
ALK5 Inhibitor IV cc-656 A 83-01 A83-01 |
| Description | A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)[1] |
| In Vitro | A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2]. |
| In Vivo | A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3]. |
| Cell Assay | HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay[2]. |
| Animal Admin | Mice[2] Female B6C3F1 mice used for the in vivo studies are maintained under specific pathogen-free conditions. To evaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells (1×106) are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150 μg/body) or vehicles (PBS with 0.5% DMSO) are injected into the abdominal cavity three times per week. Mice are euthanized before reaching the moribund state[2]. |
| References |
| Density | 1.27g/cm3 |
|---|---|
| Boiling Point | 590ºC at 760 mmHg |
| Molecular Formula | C25H19N5S |
| Molecular Weight | 421.51700 |
| Flash Point | 310.6ºC |
| Exact Mass | 421.13600 |
| PSA | 87.72000 |
| LogP | 5.78680 |
| Index of Refraction | 1.706 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302-H315-H319-H335 |
| Precautionary Statements | P280-P301 + P312 + P330-P305 + P351 + P338-P337 + P313 |
| RIDADR | NONH for all modes of transport |