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TAK-441 

Cat. No. M27901
TAK-441  Structure
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Biological Activity

TAK-441 is a highly potent and orally active hedgehog (Hh) signaling inhibitor with an IC50value of 4.4 nM. TAK-441 has strong antitumor activity in solid tumors.

Chemical Information
Molecular Weight 576.56
Formula C28H31F3N4O6
CAS Number 1186231-83-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jonathan Goldman, et al. Clin Cancer Res. Phase I dose-escalation trial of the oral investigational Hedgehog signaling pathway inhibitor TAK-441 in patients with advanced solid tumors

[2] Tsuyoshi Ishii, et al. Eur J Pharmacol. Inhibition mechanism exploration of investigational drυg TAK-441 as inhibitor against Vismodegib-resistant Smoothened mutant

[3] Naokazu Ibuki, et al. Int J Cancer. TAK-441, a novel investigational smoothened antagonist, delays castration-resistant progression in prostate cancer by disrupting paracrine hedgehog signaling

[4] Tomohiro Ohashi, et al. Bioorg Med Chem. Discovery of the investigational drυg TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: modification of the core skeleton for improved solubility

[5] Jean Y Tang, et al. Semin Cutan Med Surg. Emerging treatments and signaling pathway inhibitors

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Abmole Inhibitor Catalog




Keywords: TAK-441  supplier, Hedgehog, inhibitors, activators

 
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