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TAK-441 is an orally active inhibitor of Hedgehog signaling(IC50 = 4.4 nM) with potent antitumor activity. TAK-441 suppresses transcription factor Gli1 mRNA expression and tumor growth.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $100 | In Stock | In Stock | |
| 5 mg | $247 | In Stock | In Stock | |
| 10 mg | $372 | In Stock | In Stock | |
| 25 mg | $668 | In Stock | In Stock | |
| 50 mg | $993 | In Stock | In Stock |
| Description | TAK-441 is an orally active inhibitor of Hedgehog signaling(IC50 = 4.4 nM) with potent antitumor activity. TAK-441 suppresses transcription factor Gli1 mRNA expression and tumor growth. |
| In vitro | TAK-441 (0.03 nM–1 μM) inhibits Gli1 mRNA in the tumor and skin with IC50s of 45.7 and 113 μg/ml, respectively[3]. In LNCaP cells, TAK-441 (0.5-500 nM) delays the castration-resistant progression without affecting androgen withdrawal-induced Shh up-regulation or cell viability[4]. |
| In vivo | In ptc1+/-p53-/- mice, oral administration of TAK-441 (1-25 mg/kg) shows strong and dose-dependent antitumor activity. In BALB/c-nu/nu mice, oral administration of TAK-441 (10-100 mg/kg) shows favorable exposure and good oral absorption[4]. |
| Synonyms | TAK441 |
| Molecular Weight | 576.56 |
| Formula | C28H31F3N4O6 |
| Cas No. | 1186231-83-3 |
| Smiles | O(CC(F)(F)F)C=1C2=C(N(C)C1C(NC3CCN(C(CO)=O)CC3)=O)C=C(CC)N(CC(=O)C4=CC=CC=C4)C2=O |
| Relative Density. | 1.40 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (78.05 mM), Sonication is recommended. H2O: Insoluble | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.47 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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