2. TGF-beta/Smad
  3. TGF-β Receptor
  4. TP-008

TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.

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

TP-008 Chemical Structure

TP-008 Chemical Structure

CAS No. : 1976038-41-1

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Based on 1 publication(s) in Google Scholar

TP-008 Related Antibodies

Top Publications Citing Use of Products

View All TGF-β Receptor Isoform Specific Products:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • Biological Activity

  • Purity & Documentation

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Description

TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].

IC50 & Target

IC50: ALK 5[1]
In Vitro

TP-008 at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC50 value of 2.2?μM[1].

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

TP-008 Related Antibodies
In Vivo

TP-008 (oral administation; 50, 150 and 500 mg/kg; 5 days) induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves[1].

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

Animal Model: Rats[1]
Dosage: 50, 150 and 500 mg/kg
Administration: Oral administation; 50, 150 and 500 mg/kg; 5 days
Result: Induced cardiovalvulopathy in both the medium and high dose animal groups.
Molecular Weight

411.82

Formula

C20H15ClFN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)CN(C1=C2C=CN=C1)C(N2C3=CC(C4=CC(Cl)=CC=C4F)=NC=C3C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 9.6 mg/mL (23.31 mM; Need ultrasonic and warming; 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 2.4282 mL 12.1412 mL 24.2825 mL
5 mM 0.4856 mL 2.4282 mL 4.8565 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. 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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. 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 2.4282 mL 12.1412 mL 24.2825 mL 60.7061 mL
5 mM 0.4856 mL 2.4282 mL 4.8565 mL 12.1412 mL
10 mM 0.2428 mL 1.2141 mL 2.4282 mL 6.0706 mL
15 mM 0.1619 mL 0.8094 mL 1.6188 mL 4.0471 mL
20 mM 0.1214 mL 0.6071 mL 1.2141 mL 3.0353 mL
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TP-008 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:

TP-0081976038-41-1TP008TP 008TGF-β ReceptorTransforming growth factor beta receptorscardiovasculartoxicityInhibitorinhibitorinhibit

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