328998-53-4
328998-53-4 structure
- Name: inS3-54A18
- Chemical Name: inS3-54A18
- CAS Number: 328998-53-4
- Molecular Formula: C23H16ClNO2
- Molecular Weight: 373.832
- Catalog: Research Areas Cancer
- Create Date: 2018-04-03 11:48:04
- Modify Date: 2024-09-12 14:19:55
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inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.
| Name | inS3-54A18 |
|---|---|
| Synonyms |
2H-Pyrrol-2-one, 3-[(4-chlorophenyl)methylene]-1,3-dihydro-1-(4-hydroxyphenyl)-5-phenyl-, (3E)-
(3E)-3-(4-Chlorobenzylidene)-1-(4-hydroxyphenyl)-5-phenyl-1,3-dihydro-2H-pyrrol-2-one |
| Description | inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties. |
|---|---|
| Related Catalog | |
| Target |
STAT3 |
| In Vitro | inS3-54A18 (5 μM) reduces wound healing to 64% and 76% for A549 and MDA-MB-231 cells, respectively. inS3-54A18 at 10 μM further reduces the healing to 47% and 39%, respectively. inS3-54A18 inhibits the expression of STAT3 downstream target genes and the binding of STAT3 to its endogenous target sequences. inS3-54A18 does not affect the constitutive or IL-6-induced STAT3 activation (Tyr705 phosphorylation) but represses STAT3 target gene (survivin) expression[1]. |
| In Vivo | inS3-54A18 (200 mg/kg, p.o.) inhibits tumor growth, metastasis and expression of STAT3 target genes in a mouse xenograft model of A549 cells[1]. |
| Animal Admin | Briefly, 5×106 A549 cells are injected subcutaneously in the flanks of 5-6-week-old male NOD/SCID mice. When the tumor volume reach about 50.0 mm3, the mice are randomized using online program into two different groups (6/group) with one group treated by formulation vehicle control and the other by A18 at 200 mg/kg with oral dosing 2-3 times a week for 4 weeks. One mouse in each group dies during the study and is eliminated. Tumor volume and body weight of the remaining five mice in each group are measured twice a week without blinding. On the thirty-fifth day after implant, mice are euthanized and the tumor tissues are harvested and weighed. Necropsy is also performed to determine changes in the heart, lungs, kidneys, liver and spleen. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 630.5±55.0 °C at 760 mmHg |
| Molecular Formula | C23H16ClNO2 |
| Molecular Weight | 373.832 |
| Flash Point | 335.1±31.5 °C |
| Exact Mass | 373.086945 |
| LogP | 5.37 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.718 |
| Storage condition | 2-8℃ |