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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 2725056-38-0
分子式: C₂₃H₂₇N₇O
分子量:417.51

保管条件:

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

Data Sheet (274 KB)

ALK5-IN-79 構造式

CAS 番号: 2725056-38-0

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Fluorescent Dye

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

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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.

体内実験

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

化学情報

CAS 番号 2725056-38-0
分子量 417.51
分子式 C₂₃H₂₇N₇O
SMILES

O=C(C)N1CCC(CC1)CCN2N=C(C3=C2N=CN=C3N)C4=CC=C5NC=C(C)C5=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

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MOQ

Minimum order quantity

100 mg

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