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TAK-441

Catalog No. T21325 CAS 1186231-83-3

Synonyms: TAK441

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.

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TAK-441, CAS 1186231-83-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 132.00
5 mg	In stock	$ 328.00
10 mg	In stock	$ 563.00
25 mg	In stock	$ 890.00
50 mg	In stock	$ 1,230.00
100 mg	In stock	$ 1,670.00

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Purity: 98.79%

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

H2O: Insoluble

References and Literature

1. Goldman J, et al. Phase 1 Dose-Escalation Trial of the Oral Investigational Hedgehog Signaling Pathway Inhibitor TAK-441 in Patients with Advanced Solid Tumors. Clin Cancer Res. 2014 Dec 12. 2. Naokazu Ibuki, et al. TAK-441, a novel investigational smoothened antagonist, delays castration-resistant progression in prostate cancer by disrupting paracrine hedgehog signaling. Int J Cancer. 2013 Oct 15;133(8):1955-66. 3. Kogame A, et al. Pharmacokinetic and pharmacodynamic modeling of hedgehog inhibitor TAK-441 for the inhibition of Gli1 messenger RNA expression and antitumor efficacy in xenografted tumor model mice. Drug Metab Dispos. 2013 Apr;41(4):727-34. 4. Tomohiro Ohashi, et al. Discovery of the investigational drug 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. Bioorg Med Chem. 2012

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Stem Cell Differentiation Compound Library Anti-Cancer Compound Library Clinical Compound Library

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Keywords

TAK-441 1186231-83-3 GPCR/G Protein Stem Cells Hedgehog/Smoothened TAK441 TAK 441 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.