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

Talmapimod (Synonyms: SCIO-469)

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

Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.

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

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Description

Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.

IC50 & 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.

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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