2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. ALK5-IN-87

ALK5-IN-87 is a potent lung-restricted ALK5 inhibitor with a pKi of 10.13. ALK5-IN-87 exerts antifibrotic activity in a mouse model of lung fibrosis. ALK5-IN-87 can be used for the research of idiopathic pulmonary fibrosis.

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

ALK5-IN-87

ALK5-IN-87 Chemical Structure

CAS No. : 2921605-02-7

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ALK5-IN-87 Related Antibodies

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Description

ALK5-IN-87 is a potent lung-restricted ALK5 inhibitor with a pKi of 10.13. ALK5-IN-87 exerts antifibrotic activity in a mouse model of lung fibrosis. ALK5-IN-87 can be used for the research of idiopathic pulmonary fibrosis[1].

In Vitro

ALK5-IN-87 (compound 20) inhibits TGF-β1-induced pSMAD2 phosphorylation in A549 cells with a pIC50 of 7.28[1].
ALK5-IN-87 inhibits TGF-β1-induced pSMAD2 phosphorylation in human lung fibroblasts with a pIC50 of 7.69[1].
ALK5-IN-87 potently inhibits purified ALK4 kinase domain with a pKi of 9.86[1].

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

ALK5-IN-87 Related Antibodies
Parmacokinetics
Species Dose Route CLplasma Vdss T1/2
Mice[1] 2 mg/kg i.v. 70 mL/min/kg 5.2 L/kg 1.7 h
In Vivo

ALK5-IN-87 (compound 20) (0.3-1 mg/kg; i.n.; once daily; starting at day 7 until day 21) exerts antifibrotic activity in a mouse model of lung fibrosis[1].

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

Animal Model: C57BL/6J mice (7-8 weeks old) with Bleomycin (BLM) (HY-17565)-induced lung fibrosis[1]
Dosage: 0.3; 1 mg/kg
Administration: i.n.; once daily; starting at day 7 until day 21
Result: Significantly slowed down the decline in forced vital capacity (FVC) value by 43% at 1 mg/kg, ompared to BLM group.
Did not result in an increased efficacy compared to the
lower dose of 1 mg/kg at 0.3 mg/kg.
Induced a significant decrease by 23% in the Ashcroft score compared to the vehicle/BLM-treated animals at 1 mg/kg.
Showed antifibrotic activity.
Molecular Weight

546.06

Formula

C25H29ClFN7O2S
CAS No.
SMILES

O=C(NC1=NC=CC(NC2=CC(C3=CC(Cl)=CC=C3F)=NN=C2SCCO)=C1)CCN4CCN(C)CC4
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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ALK5-IN-87 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.

Keywords:

ALK5-IN-872921605-02-7Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246A549 cellsDDR1ALK4TNIKmouse model of lung fibrosisTGFβ-R2ALK5p38αJNK3human lung fibroblastsInhibitorinhibitorinhibit

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