A83-01 --- an ALK inhibibitor

A-83-01 is an ALK inhibibitor. It was found that A-83-01 inhibited the transcriptional activity induced by TGF-beta type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 was found to be more potent in the inhibition of ALK5 than a previously described ALK-5 inhibitor, SB-431542, and also to prevent phosphorylation of Smad2/3 and the growth inhibition induced by TGF-beta. A-83-01 inhibited the epithelial-to-mesenchymal transition induced by TGF-beta, suggesting that A-83-01 and related molecules may be useful for preventing the progression of advanced cancers.

Product information

CAS Number: 909910-43-6

Molecular Weight: 421.52

Formula: C25H19N5S

Chemical Name: 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide

Smiles: CC1=CC=CC(=N1)C1=NN(C=C1C1=CC=NC2=CC=CC=C12)C(=S)NC1C=CC=CC=1

InChiKey: HIJMSZGHKQPPJS-UHFFFAOYSA-N

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)

Technical Data

Appearance: white solid powder

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥24 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

A83-01 is typically used at 10 µM as final concentration in cell culture.

In Vivo:

A83-01 was orally dosed to mice at 100-200 mg/kg once per day or intraperitoneally dosed to mice at 10-100 mg/kg once per day.

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. (2005) Cancer Science 96 (11), 791-800.
2. i W, et al. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. (2009) Cell Stem Cell 4(1), 16-19.
3. Yuan X, et al. Combined Chemical Treatment Enables Oct4-Induced Reprogramming from Mouse Embryonic Fibroblasts. (2011) Stem Cells 29(3), 549¨C553.
4. Klincumhom N, et al. Selective TGF-β1/ALK inhibitor improves neuronal differentiation of mouse embryonic stem cells. (2014) Neurosci Lett. 578:1-6.

Products are for research use only. Not for human use.