Free shipping on all orders over $ 500

A 83-01

Cat. No. M5037
A 83-01 Structure
Synonym:

A83-01; A-83-01

Size Price Availability Quantity
2mg USD 40  USD40 In stock
5mg USD 60  USD60 In stock
10mg USD 100  USD100 In stock
50mg USD 300  USD300 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation.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 compound accumulation of F-SL in the tumor than liposome alone at 24 h post injection.

*The compound is unstable in solutions, freshly prepared is recommended



Product Citations
Customer Product Validations & Biological Datas
Source Breast Cancer Res Treat (2017). Figure 6. A 83-01
Method MTT assay
Cell Lines SKBR3 cells
Concentrations 1 μM 
Incubation Time 16 h
Results As shown in Fig. 6c that A83-01 alone reduced approximately 17% cell migration of JIMT1 and trastuzumab alone inhibited 20% cell migration, while in combination of A83-01 and trastuzumab synergistically inhibited JIMT1 cell migration up to 90%.
Chemical Information
Molecular Weight 421.52
Formula C25H19N5S
CAS Number 909910-43-6
Solubility (25°C) DMSO 24 mg/mL
Storage -20°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Furutani Y,et.al. J Cell Biochem. Role of endogenous TGF-β family in myogenic differentiation of C2C12 cells.

[2] Taniguchi Y,et.al. Cancer Sci. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor.

[3] Masayoshi Tojo, et al. Cancer Sci. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta

Related TGF-β Receptor Products
GW-6604 

GW-6604 is an ALK5 inhibitor with an IC50 value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis.

SB-505124 hydrochloride 

SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

Isosaponarin

Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin increases collagen synthesis, caused by up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production.

PF-06952229 

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer.

Chromenone 1 

Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.

  Catalog
Abmole Inhibitor Catalog




Keywords: A 83-01, A83-01; A-83-01 supplier, TGF-β Receptor, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.