2. TGF-beta/Smad
  3. TGF-β Receptor
  4. 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.

For research use only. We do not sell to patients.

THRX-144644 Chemical Structure

THRX-144644 Chemical Structure

CAS No. : 2442519-59-5

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Based on 1 publication(s) in Google Scholar

THRX-144644 Related Antibodies

Top Publications Citing Use of Products

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

THRX-144644 Related Antibodies
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.
Appearance

Solid

Color

White to off-white

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

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (97.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9531 mL 9.7656 mL 19.5312 mL
5 mM 0.3906 mL 1.9531 mL 3.9062 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9531 mL 9.7656 mL 19.5312 mL 48.8281 mL
5 mM 0.3906 mL 1.9531 mL 3.9062 mL 9.7656 mL
10 mM 0.1953 mL 0.9766 mL 1.9531 mL 4.8828 mL
15 mM 0.1302 mL 0.6510 mL 1.3021 mL 3.2552 mL
20 mM 0.0977 mL 0.4883 mL 0.9766 mL 2.4414 mL
25 mM 0.0781 mL 0.3906 mL 0.7812 mL 1.9531 mL
30 mM 0.0651 mL 0.3255 mL 0.6510 mL 1.6276 mL
40 mM 0.0488 mL 0.2441 mL 0.4883 mL 1.2207 mL
50 mM 0.0391 mL 0.1953 mL 0.3906 mL 0.9766 mL
60 mM 0.0326 mL 0.1628 mL 0.3255 mL 0.8138 mL
80 mM 0.0244 mL 0.1221 mL 0.2441 mL 0.6104 mL
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THRX-144644 Related Classifications

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.

Keywords:

THRX-1446442442519-59-5THRX144644THRX 144644TGF-β ReceptorTransforming growth factor beta receptorslung-selectiveTGFβBEAS2B cell linesystemic toxicitiesInhibitorinhibitorinhibit

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