DC Chemicals Limited
China
Product Name: SCIO-469
Price: $500.0/100mg $1000.0/250mg $2000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

309913-83-5

309913-83-5 structure

Name: Talmapimod
Chemical Name: 2-[6-chloro-5-[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine-1-carbonyl]-1-methylindol-3-yl]-N,N-dimethyl-2-oxoacetamide
CAS Number: 309913-83-5
Molecular Formula: C₂₇H₃₀ClFN₄O₃
Molecular Weight: 513.003
Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
Create Date: 2018-07-20 02:23:57
Modify Date: 2024-01-02 02:58:51
Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.

Name	2-[6-chloro-5-[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine-1-carbonyl]-1-methylindol-3-yl]-N,N-dimethyl-2-oxoacetamide
Synonyms	1H-Indole-3-acetamide, 6-chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo- SCIO-469 Scios 469 2-(6-Chloro-5-{[(2R,5S)-4-(4-fluorobenzyl)-2,5-dimethyl-1-piperazinyl]carbonyl}-1-methyl-1H-indol-3-yl)-N,N-dimethyl-2-oxoacetamide Talmapimod

Description	Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK Research Areas >> Cancer
Target	IC50: 9 nM (p38)[1].
In Vitro	Talmapimod (SCIO-469)decreased constitutive p38α MAPK phosphorylation of both 5T2MM and 5T33MM cells. Talmapimod (SCIO-469) also inhibits secretion and expression of the osteoclast-activating factors IL-11, receptor activator of NF-κB ligand, and macrophage inflammatory protein 1α, and prevents human osteoclast activationIn. It can also inhibit multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.
In Vivo	Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.
Cell Assay	5TMM cells (0.5 × 106/mL) were pretreated with different concentrations of Talmapimod (SCIO-469) in serum-free medium and then placed in the lower compartment of a Transwell system. Syngeneic bone marrow stromal cells were seeded into the Transwell itself. After 18 h, the 5TMM cells were collected from the lower compartment and stained for active caspase-3 with a FITC-labeled antibody according to manufacturer's instructions
Animal Admin	Animal injection[1] For studies of the effect of Talmapimod (SCIO-469) on myeloma development, three groups of male mice (n = 12) were injected i.v. with 0.5 × 106 5T33MM cells. Mice were left untreated (naive) or, if injected with tumor cells, treated from the time of tumor cells injection with either Talmapimod (SCIO-469) (150 or 450 mg/kg powder diet continuously available for the mice) or a vehicle (PBS) until the first mice showed signs of morbidity (at 3.7 weeks).
References	[1]. Hideshima T et al. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 2004 Nov 18, 23(54), 8766-76. [2]. Vanderkerken K et al. Inhibition of p38alpha mitogen-activated protein kinase prevents the development of osteolytic bone disease,reduces tumor burden, and increases survival in murine models of multiple myeloma. Vanderkerken K et al.

Density	1.3±0.1 g/cm3
Boiling Point	658.0±65.0 °C at 760 mmHg
Molecular Formula	C₂₇H₃₀ClFN₄O₃
Molecular Weight	513.003
Flash Point	351.7±34.3 °C
Exact Mass	512.199036
PSA	65.86000
LogP	2.73
Vapour Pressure	0.0±2.0 mmHg at 25°C
Index of Refraction	1.619