1116235-97-2

Basic information

• Product Name: GSK1838705A
• Synonyms: GSK1838705;2-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-6-fluoro-N-methylbenzamide;2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide GSK1838705A;2-[[2-[[1-[2-(Dimethylamino)acetyl]-2,3-dihydro-5-methoxy-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methy;GSK1838705A;2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide;2-[[2-[[1-[2-(Dimethylamino)acetyl]-2,3-dihydro-5-methoxy-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide
• CAS NO: 1116235-97-2
• Molecular Formula: C₂₇H₂₉FN₈O₃
• Molecular Weight: 532.5693632
• Product Categories: Inhibitors
• Mol File: 1116235-97-2.mol
• Article Data: 1

Chemical Properties

• Appearance: white to light brown/
• Density: 1.399
• Storage Temp.: ?20°C
• Solubility: DMSO: soluble20mg/mL, clear
• PKA: 13.27±0.50(Predicted)
• CAS DataBase Reference: GSK1838705A(CAS DataBase Reference)
• NIST Chemistry Reference: GSK1838705A(1116235-97-2)
• EPA Substance Registry System: GSK1838705A(1116235-97-2)

Safety Data

• WGK Germany: 3
• Hazardous Substances Data: 1116235-97-2(Hazardous Substances Data)

Usage

Uses

GSK 1838705 is a potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK).

Biological Activity

gsk1838705a is a small-molecule kinase inhibitor that inhibits igf-ir and the insulin receptor with ic50s of 2.0 and 1.6 nmol/l, respectively.igf-1r is a transmembrane receptor which is activated by insulin-like growth factor 1 and by a related hormone igf-2. this protein plays important role in the regulation of development. the insulin receptor is also a transmembrane receptor that is activated by insulin, igf-1 and igf2. this receptor is involved in insulin signaling pathway and plays an essential role in the regulation of glucose homeostasis.gsk1838705a obstructs the in vitro expansion of cell lines got from strong and hematologic malignancies, including numerous myeloma and ewing's sarcoma, and hinders the development of human tumor xenografts in vivo. in spite of the inhibitory impact of gsk1838705a on insulin receptor, insignificant effects on glucose homeostasis were seen at efficacious dosages. gsk1838705a represses the anaplastic lymphoma kinase (alk), which drives the distorted development of anaplastic substantial cell lymphomas, some neuroblastomas, and a subset of non–small cell lung growths.gsk1838705a restrains alk, with an ic50 value of 0.5 nm, furthermore, causes complete relapse of alk-ward tumors in vivo at very-endured measurements. gsk1838705a arrives for a promising antitumor agent for helpful use in human growth.

references

[1]. sabbatini p, et al. gsk1838705a inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. mol cancer ther. 2009 oct;8(10):2811-20.

Upstream product

• 1116236-02-2 2-({2-{[1-(N,N-dimethylglycyl)-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino}-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)-6-fluoro-N-methylbenzamide 

Relevant articles and documents

2- [ (2-{PHENYLAMINO}-1H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) AMINO] BENZAMIDE DERIVATIVES AS IGF-1R INHIBITORS FOR THE TREATMENT OF CANCER

Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.