1. TGF-beta/Smad
    Protein Tyrosine Kinase/RTK
  2. TGF-β Receptor
    ALK

A 83-01 

Cat. No.: HY-10432 Purity: >97.0%
Data Sheet SDS Handling Instructions

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, 45 and 7.5 nM, respectively.

For research use only. We do not sell to patients.
A 83-01 Chemical Structure

A 83-01 Chemical Structure

CAS No. : 909910-43-6

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10 mg $90 In-stock
50 mg $280 In-stock
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Description

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, 45 and 7.5 nM, respectively.

IC50 & Target

IC50: 12 nM (ALK5), 45 nM (ALK4), 7.5 nM (ALK7)

In Vitro

A-83-01 (4 µM) treatment increases myotube formation, the expression of MyHC and the expression of Myf5 and MyoD in C2C12 cells[1]. Expression of pSmad3 is increased by the addition of TGF-β1, and the effects of TGF-β1 are inhibited in ovarian cancer cells by A-83-01. TGF-β1 increases cell motility, adhesion and invasion, while A-83-01 decreases these behaviors in HM-1 cells[2]. A-83-01 treatment significantly increases these parameters within 24 h that is positively related to pericyte coverage and tumor cell proliferation. Apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging is decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure[3].

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 stronger antitumor effect in mice bearing M109 cells[4].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3724 mL 11.8618 mL 23.7237 mL
5 mM 0.4745 mL 2.3724 mL 4.7447 mL
10 mM 0.2372 mL 1.1862 mL 2.3724 mL
Cell Assay
[2]

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 following the manufacturer's instructions. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

A 83-01 is formulated in PBS with 0.5% DMSO.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

421.52

Formula

C₂₅H₁₉N₅S

CAS No.

909910-43-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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A 83-01
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HY-10432
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