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

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TP-008 Chemical Structure

TP-008 Chemical Structure

CAS No. : 1976038-41-1

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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.

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.
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

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

Purity & Documentation
References
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TP-008 Related Classifications

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  • 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:
TP-008
Cat. No.:
HY-125851
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