CAS 909910-43-6|A 83-01

Introduction：Basic information about CAS 909910-43-6|A 83-01, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. A 83-01 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	A 83-01
CAS Number	909910-43-6	Molecular Weight	421.51700
Density	1.27g/cm3	Boiling Point	590ºC at 760 mmHg
Molecular Formula	C₂₅H₁₉N₅S	Melting Point	/
MSDS	ChineseUSA	Flash Point	310.6ºC
Symbol	GHS07	Signal Word	Warning

Names

Name	3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
Synonym	More Synonyms

A 83-01 BiologicalActivity

Description	A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.
Related Catalog	Signaling Pathways >>TGF-beta/Smad >>TGF-β ReceptorResearch Areas >>Cancer
Target	IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)[1]
In Vitro	A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2].
In Vivo	A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3].
Cell Assay	HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay[2].
Animal Admin	Mice[2] Female B6C3F1 mice used for the in vivo studies are maintained under specific pathogen-free conditions. To evaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells (1×106) are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150 μg/body) or vehicles (PBS with 0.5% DMSO) are injected into the abdominal cavity three times per week. Mice are euthanized before reaching the moribund state[2].
References	[1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800. [2]. Yamamura S, et al. 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]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.

Chemical & Physical Properties

Density	1.27g/cm3
Boiling Point	590ºC at 760 mmHg
Molecular Formula	C₂₅H₁₉N₅S
Molecular Weight	421.51700
Flash Point	310.6ºC
Exact Mass	421.13600
PSA	87.72000
LogP	5.78680
Index of Refraction	1.706
InChIKey	HIJMSZGHKQPPJS-UHFFFAOYSA-N
SMILES	Cc1cccc(-c2nn(C(=S)Nc3ccccc3)cc2-c2ccnc3ccccc23)n1

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H315-H319-H335
Precautionary Statements	P280-P301 + P312 + P330-P305 + P351 + P338-P337 + P313
RIDADR	NONH for all modes of transport

Synonyms

A-83-01

ALK5 Inhibitor IV

cc-656

A 83-01

A83-01

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