| Identification | Back Directory | [Name]
GSK1838705A | [CAS]
1116235-97-2 | [Synonyms]
CS-236
GSK1838705
GSK1838705A
GSK1838705A USP/EP/BP
GSK1838705A >=98% (HPLC)
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-[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
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
Benzamide, 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-methyl-
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-[(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 | [Molecular Formula]
C27H29FN8O3 | [MDL Number]
MFCD19443644 | [MOL File]
1116235-97-2.mol | [Molecular Weight]
532.57 |
| Chemical Properties | Back Directory | [density ]
1.399 | [storage temp. ]
?20°C | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
powder | [pka]
13.27±0.50(Predicted) | [color ]
white to light brown | [InChIKey]
HZTYDQRUAWIZRE-UHFFFAOYSA-N | [SMILES]
C(NC)(=O)C1=C(F)C=CC=C1NC1N=C(NC2=CC3=C(C=C2OC)CCN3C(CN(C)C)=O)N=C2NC=CC2=1 |
| Hazard Information | Back Directory | [Uses]
GSK 1838705 is a potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK). | [Definition]
ChEBI: 2-[[2-[[1-[2-(dimethylamino)-1-oxoethyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide is an organooxygen compound and an organonitrogen compound. It is functionally related to an alpha-amino acid. | [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. | [in vivo]
GSK1838705A shows robust antitumor activity in animal xenograft models. Tumor types likely to respond to GSK1838705A include multiple myeloma and Ewing's sarcoma, as well as ALK-driven tumors (e.g., ALCL, NSCLC, and neuroblastoma). A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg results in 35% and 65% inhibition of IGF-IR phosphorylation, respectively, whereas doses ≥1 mg/kg results in complete inhibition of ligand-induced IGF-IR phosphorylation[1]. | [storage]
Store at -20°C | [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. |
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| Company Name: |
China Langchem Inc.
|
| Telephone: |
0086-21-58956006 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList19141/0_EN.htm |
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
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