N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide
- Product Name
- N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide
- CAS No.
- 1333146-24-9
- Chemical Name
- N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide
- Synonyms
- CS-2064;CS-4936;ILK-IN-1;OSU-T315;GTPL8116;BDBM50353484;CHEMBL1830587;SCHEMBL8536228;OSU-T315 analog;OSU-T315 (OSU-T 315)
- CBNumber
- CB22743020
- Molecular Formula
- C30H30F3N5O
- Formula Weight
- 533.59
- MOL File
- 1333146-24-9.mol
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide Property
- Boiling point:
- 739.2±60.0 °C(Predicted)
- Density
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 10mM
- form
- A solid
- pka
- 16.02±0.46(Predicted)
- color
- White to light yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- CS-5471
- Product name
- ILK-IN-2
- Purity
- 99.41%
- Packaging
- 2mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-5471
- Product name
- ILK-IN-2
- Purity
- 99.41%
- Packaging
- 5mg
- Price
- $380
- Updated
- 2021/12/16
- Product number
- CS-5471
- Product name
- ILK-IN-2
- Purity
- 99.41%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- orb573462
- Product name
- OSU-T315
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1133.9
- Updated
- 2021/12/16
- Product number
- orb573462
- Product name
- OSU-T315
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1802
- Updated
- 2021/12/16
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide Chemical Properties,Usage,Production
Uses
ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models[1][2].
in vivo
ILK-IN-2 (25-50 mg/kg, oral or intraperitoneal injection, once daily, 2-4 weeks) delays leukemia progression in mice and significantly improves the overall survival rate of mice harboring TCL1 leukemia cells[ 1 ].
ILK-IN-2 (25-50 mg/kg, orally, daily, for 35 days) inhibits the growth of PC-3 xenograft tumors in nude mice[2].
| Animal Model: | Pharmacokinetic properties of OSU-T315[1] |
| Dosage: | 50 mg/kg, daily for 4 weeks; 25 mg/kg, once daily for 2 weeks |
| Administration: | Oral; Intraperitoneal injection (i.p.) |
| Result: | Reduced white blood cell count and prolonged the survival of mice. |
| Animal Model: | PC-3 tumor xenograft mice model[2] |
| Dosage: | 25, 50 mg/kg; daily; 35 days |
| Administration: | Oral |
| Result: | Significantly inhibited tumor growth (25 and 50 mg/kg groups inhibited 48% and 62% respectively). Showed that the phosphorylation of Ser-473-Akt was dose-dependently inhibited, while the phosphorylation of Thr-308-Akt was not affected. At the same time, the phosphorylation levels of GSK3β and MLC and the expression levels of YB-1, HER2 and EGFR also appeared in parallel decline. |
IC 50
ILK: 0.6 μM (IC50)
References
[1] Ta-Ming Liu, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. DOI:10.1182/blood-2014-06-583518
[2] Su-Lin Lee, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. DOI:10.1021/jm2007744
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide Preparation Products And Raw materials
Raw materials
Preparation Products
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