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909910-43-6 (A 83-01)

1

Identification

A 83-01 A 83-01
Name A 83-01
Formula C25H19N5S
MW 421.52
CAS No. 909910-43-6
EINECS
Smiles S=C(N1N=C(C2=NC(C)=CC=C2)C(C3=CC=NC4=CC=CC=C34)=C1)NC5=CC=CC=C5
Synonyms A83-01;A-83-01; 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
InChI InChI=1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)
2

Introduction

A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).

Background Information

Selective inhibitor of TGF-β type I receptor ALK5 kinase type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 ; transforming growth factor (TGF)-β inhibitor ......by AOBIOUS INC
A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). IC50 Value: 12 nM ( ALK5) Target: ALK5 A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. A 83-01 only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity and is more potent than SB 431542. in vitro: A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation [1]. Microarray analysis of HM-1 cells treated with TGF-β1 and/or A-83-01 revealed that A-83-01 efficiently inhibited transcriptional changes that are induced by TGF-β1 [2]. -83-01 treatment significantly increased these parameters within 24 h that was positively related to pericyte coverage and tumor cell proliferation. Furthermore, apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging was decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure. Vascular function of the tumor improved by A-83-01treatment well assessed on post-Gd-L-enhanced MR images [3]. in vivo: The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3 h post injection. A-83-01 induced 1.7-fold higher drug accumulation of F-SL in the tumor than liposome alone at 24 h post injection [4]. ......by MedChemexpress Co., Ltd.
A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 nM, 45 nM and 7.5 nM, respectively. ......by Target Molecule Corp.
Potent inhibitor of TGF-<span class='symbol'>&beta;</span> type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC<sub>50</sub> values are 12, 45 and 7.5 nM respectively). Blocks phosphorylation of Smad2 and inhibits TGF-<span class='symbol'>&beta;</span>-induced epithelial-to-mesenchymal transition. Only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. More potent than <a href='dispprod.php?ItemId=54518'>SB 431542</a> (Cat.No. 1614). Inhibits differentiation of rat induced pluripotent stem cells (riPSCs) and increases clonal expansion efficiency. Helps maintain homogeneity and long-term <em>in vitro</em> self-renewal of human iPSCs. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000024318

Storage condition

Store at -20&deg;C by Tocris Bioscience Inc.

Solubility

DMSO by MedChemexpress Co., Ltd.
Soluble to 50 mM in DMSO by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Protein Tyrosine Kinase/RTK TGF-beta/Smad
Target ALK TGF-β Receptor
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
A 83-01 - Not Found
A 83-01 - No Development Reported
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Safety Data of A 83-01

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD11() USA
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 10mg/USD90(In stock);50mg/USD280(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD140(In stock);50mg/USD405(In stock) China
Target Molecule Corp. 2mg/USD50();5mg/USD88();10mg/USD156();25mg/USD248();50mg/USD458() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 909910-43-6

Name CAS No Formula MW

Recommended Compounds in ALK TGF-β Receptor

Name CAS No Formula MW
PF-06463922 1454846-35-5 C21H19FN6O2 406.41
CEP-37440 1391712-60-9 C30H38ClN7O3 580.12
HG-14-10-04 1356962-34-9 C29H34ClN7O 532.08
LDK378 (dihydrochloride) 1380575-43-8 C28H38Cl3N5O3S 631.06
LDK378 1032900-25-6 C28H36ClN5O3S 558.14
AZD-3463 1356962-20-3 C24H25ClN6O 448.95
X-376 1365267-27-1 C25H25Cl2FN6O3 547.41
CEP-28122 1022958-60-6 C28H35ClN6O3 539.07
AP26113 1197958-12-5 C26H34ClN6O2P 529.01
Crizotinib (hydrochloride) 1415560-69-8 C21H23Cl3FN5O 486.8
ALK inhibitor 2 761438-38-4 C23H28ClN7O3S 518.03
ALK inhibitor 1 761436-81-1 C23H28BrN7O3S 562.48
1-Piperidineacetamide, 4-[3-methoxy-4-[[7-(2-methoxyphenyl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]- 1233145-49-7 C27H30N6O3 486.57
ASP3026 1097917-15-1 C29H40N8O3S 580.74
GSK1838705A 1116235-97-2 C27H29FN8O3 532.57
CH5424802 1256580-46-7 C30H34N4O2 482.62
Crizotinib 877399-52-5 C21H22Cl2FN5O 450.34
NVP-TAE 684 761439-42-3 C30H40ClN7O3S 614.2
Belizatinib 1357920-84-3 C33H44FN5O3 577.73
Brigatinib 1197953-54-0 C29H39ClN7O2P 584.09

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

[1]. Furutani Y, Umemoto T, Murakami M, Role of endogenous TGF-β family in myogenic differentiation of C2C12 cells. J Cell Biochem. 2011 Feb;112(2):614-24.

[2]. Yamamura S, Matsumura N, Mandai M, The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.

[3]. Kawano K, Maitani Y. Tumor permeability of nanocarriers observed by dynamic contrast-enhanced magnetic resonance imaging. Yakugaku Zasshi. 2010 Dec;130(12):1679-85.

[4]. Taniguchi Y, Kawano K, Minowa T, Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.

Protocol Reference

Tojo et al (2005) The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer.Sci. 96 791. PMID: 16271073.

Hoberg et al (2008) Attachment to laminin-111 facilitates transforming growth factor β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts. Ann.Rheum.Dis. 66 446.

Li et al (2009) Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4 16. PMID: 19097958.

......by Tocris Bioscience Inc.
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More Information

A 83-01

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