1. TGF-beta/Smad
  2. TGF-β Receptor
  3. THRX-144644

THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.

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THRX-144644 Chemical Structure

THRX-144644 Chemical Structure

CAS No. : 2442519-59-5

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Description

THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition[1].

IC50 & Target[1]

ALK5

0.14 nM (IC50)

In Vitro

THRX-144644 (1-10000 nM; 1 h) inhibits ALK5 with an IC50 value of 23 nM in human BEAS2B cell line.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

THRX-144644 (2-60 mg/kg; Inhalation: nebulizer, daily, for 14 days) is a Lung-selective inhibitor and targets to the lungs in Sprague Dawley rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley rats[1]
Dosage: 2, 10, and 60 mg/kg
Administration: Inhalation: nebulizer, daily, for 14 days
Result: Had the L:P ratio (AUC) was 0.44.
Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.
Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
Molecular Weight

512.00

Formula

C26H28ClF2N7

CAS No.
SMILES

FC1=CC(F)=C(C2=NNC=C2C3=NC4=C(C=C3)N=CC(NCCN5CCN(C(C)C)CC5)=C4)C=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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THRX-144644 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
THRX-144644
Cat. No.:
HY-150169
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