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.

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

ALK5-IN-79

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.

Cellular Effect
Cell Line Type Value Description References
4T1 CC50
1.66 μM
Compound: 57
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
BEAS-2B CC50
19.14 μM
Compound: 57
Cytotoxicity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Cytotoxicity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
HEK-293T CC50
> 20 μM
Compound: 57
Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
HepG2 CC50
8.67 μM
Compound: 57
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
Kasumi 1 CC50
1.92 μM
Compound: 57
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
L02 CC50
14.9 μM
Compound: 57
Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
MCF-10A CC50
13.68 μM
Compound: 57
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
MDA-MB-231 CC50
5.21 μM
Compound: 57
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
MV4-11 CC50
6.81 μM
Compound: 57
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
PANC-1 CC50
> 20 μM
Compound: 57
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
Panc02 CC50
19.28 μM
Compound: 57
Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
U-251 CC50
> 20 μM
Compound: 57
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 38626523]
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
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-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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HY-163507
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