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Cat. No.: HY-163507

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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.

CAS No.: 2725056-38-0
Formula: C₂₃H₂₇N₇O
Molecular Weight:417.51

Storage:

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

Data Sheet (274 KB)

ALK5-IN-79 Chemical Structure

CAS No.: 2725056-38-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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]
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]
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]
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.

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

Chemical Information

CAS No. 2725056-38-0
Molecular Weight 417.51
Formula C₂₃H₂₇N₇O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yubo Wang et al. Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor. European Journal of Medicinal Chemistry. Volume 271, 5 May 2024, 116395

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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