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 an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod 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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10 mM * 1 mL in DMSO USD 163 In-stock
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10 mg USD 228 In-stock
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25 mg USD 480 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 an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs[1][2][3].

IC50 & Target[1]

p38α

9 nM (IC50)

p38β

90 nM (IC50)

In Vitro

Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells[1].
Talmapimod inhibits LPS-induced TNF-a production in human whole blood[2].
Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3].

Western Blot Analysis[1]

Cell Line: MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines
Concentration: 100, 200 nM
Incubation Time: 1 hour
Result: Strongly inhibits phosphorylation of p38 MAPK.
In Vivo

Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease[2].
Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models[3].
Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination[4].

Animal Model: Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)[4]
Dosage: P.o.; twice daily orally for 14 days
Administration: 10, 30, 90 mg/kg
Result: Dose-dependently reduced tumor growth.
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
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Keywords:

TalmapimodSCIO-469SCIO469SCIO 469p38 MAPKmultiplemyelomacellsHsp27tumorcytotoxicityphosphorylationInhibitorinhibitorinhibit

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