Talmapimod (SCIO-469) (Synonyms: Talmapimod) |
| Catalog No.GC34072 |
Talmapimod (SCIO-469) (SCIO-469) es un p38α oralmente activo, selectivo y competitivo con ATP; inhibidor con una IC50 de 9 nM. Talmapimod (SCIO-469) muestra una selectividad de aproximadamente 10 veces sobre p38β y una selectividad de al menos 2000 veces sobre un panel de otras 20 quinasas, incluidas otras MAPK.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 309913-83-5
Sample solution is provided at 25 µL, 10mM.
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Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.
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.
Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.
[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.
Cell experiment: | 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 experiment: | 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. | |
| Cas No. | 309913-83-5 | SDF | |
| Sinónimos | Talmapimod | ||
| Canonical SMILES | O=C(N(C)C)C(C1=CN(C)C2=C1C=C(C(N3[C@H](C)CN(CC4=CC=C(F)C=C4)[C@@H](C)C3)=O)C(Cl)=C2)=O | ||
| Formula | C27H30ClFN4O3 | M.Wt | 513 |
| Solubility | DMSO : ≥ 100 mg/mL (194.93 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9493 mL | 9.7466 mL | 19.4932 mL |
| 5 mM | 0.3899 mL | 1.9493 mL | 3.8986 mL |
| 10 mM | 0.1949 mL | 0.9747 mL | 1.9493 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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