1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
  3. Talmapimod

Talmapimod (Synonyms: SCIO-469)

Cat. No.: HY-10406 Purity: 98.73%
Handling Instructions

Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with IC50 of 9 nM, shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

For research use only. We do not sell to patients.

Talmapimod Chemical Structure

Talmapimod Chemical Structure

CAS No. : 309913-83-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 163 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
25 mg USD 480 In-stock
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50 mg USD 804 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with IC50 of 9 nM, shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

IC50 & Target

IC50: 9 nM (p38)[1].

In Vitro

Talmapimod (SCIO-469) decreases 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[2].
Talmapimod (SCIO-469) inhibits LPS-induced TNF-a production in human whole blood[3].

In Vivo

Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease[2].

Clinical Trial
Molecular Weight

513.00

Formula

C₂₇H₃₀ClFN₄O₃

CAS No.

309913-83-5

SMILES

O=C(N(C)C)C(C1=CN(C)C2=C1C=C(C(N3[[email protected]](C)CN(CC4=CC=C(F)C=C4)[[email protected]@H](C)C3)=O)C(Cl)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (194.93 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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