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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
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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

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


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