2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. ALK5-IN-79

ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.

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ALK5-IN-79 Chemical Structure

ALK5-IN-79 Chemical Structure

CAS No. : 2725056-38-0

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ALK5-IN-79 Related Antibodies

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Description

ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.

In Vitro

ALK5-IN-79 (1000 nM; 2 h) has strong-to oderate inhibitory activities against ALK5, SRC, LCK, BRAF (V600E), RET, PDGFRα, EGFR and KDR at 1000 nM (inhibitory rate >20%) [1].
ALK5-IN-79 (0, 0.125, 0.25, 0.5, 1.0 and 2.0 μM; 1 h) inhibits the phosphorylation of smad 3, at a dose-dependent pattern[1].

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

ALK5-IN-79 Related Antibodies

Western Blot Analysis[1]

Cell Line: Abnormal proliferation of cancer associated fibroblasts
Concentration: 0-2.0 μM
Incubation Time: 1 h
Result: ALK5-IN-79 blocked the TGF-β1 induced upregulation of collagen I (Col1) and α-SMA at mRNA and protein levels, i.e., the targeted genes of samd 3. ALK5-IN-79 led to the reduced secretion of Col 1.
In Vivo

ALK5-IN-79 (300 mg/kg/day; ip; every day for 7 days) decreases the weight of the mice. ALK5-IN-79 is safe in vivo[1].
ALK5-IN-79 (10 and 50 mg/kg/day; iv; every other day for 24 days) resultes in tumor growth inhibition (TGI) rates of 61.9% and 80.5% in the Syngeneic Model, ALK5-IN-79 (10 and 50 mg/kg/day; iv; every other day for 24 days) resultes in tumor growth inhibition (TGI) rates of 62.1% and 75.6% in the PANC-1 subcutaneous xenograft model. ALK5-IN-79 inhibites pancreatic cancer tumor growth in a metrology-dependent manner[1].

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

Animal Model: Pan02 syngeneic model and PANC-1 subcutaneous xenograft mode
Dosage: 10mg/kg and 50mg/kg ; every other day for 24 days
Administration: Intravenous injection (i.v.)
Result: Inhibited the growth of pancreatic cancer tumors in a dose-dependent manner
Molecular Weight

417.51

Formula

C23H27N7O
CAS No.
SMILES

O=C(C)N1CCC(CC1)CCN2N=C(C3=C2N=CN=C3N)C4=CC=C5NC=C(C)C5=C4
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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-79 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-792725056-38-0Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Pancreatic cancerActivin receptor-like kinase 5 inhibitor TGFβ1/SMAD signaling pathwayPan02 syngeneic model and PANC-1 subcutaneous xenograft modeALK5 InhibitorInhibitorinhibitorinhibit

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