SML0995

GSK1838705A

≥98% (HPLC)

• Synonym(s): 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-methyl-benzamide
• Empirical Formula (Hill Notation): C₂₇H₂₉FN₈O₃
• CAS Number: 1116235-97-2
• Molecular Weight: 532.57
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: powder
• color: white to light brown
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: −20°C
• InChI: 1S/C27H29FN8O3/c1-29-26(38)23-17(28)6-5-7-18(23)31-25-16-8-10-30-24(16)33-27(34-25)32-19-13-20-15(12-21(19)39-4)9-11-36(20)22(37)14-35(2)3/h5-8,10,12-13H,9,11,14H2,1-4H3,(H,29,38)(H3,30,31,32,33,34)
• InChI key: HZTYDQRUAWIZRE-UHFFFAOYSA-N

Description

Application

GSK1838705A has been used as an insulin receptor inhibitor in Roswell Park memorial institute medium (RPMI) 1640 medium for inhibitor experiments, to prove that the induction of interleukin-1 β (IL-1β) is dependent on insulin receptor signaling.

Biochem/physiol Actions

GSK1838705A can be used to treat prostate cancer (PC). It is capable of decreasing the viability of docetaxel-sensitive and docetaxel-resistant prostate cancer cells. GSK1838705A can stimulate apoptosis of PC-3R cells. It is an alternative therapeutic option for crizotinib-resistant anaplastic large cell lymphoma (ALCL).

GSK1838705A is a cell penetrant anti-tumor agent that potently inhibits the insulin-like growth factor-I receptors (IGF-IR), insulin receptors (IR) and anaplastic lymphoma kinase (ALK). GSK1838705A potently inhibits cell proliferation of multiple solid and hematologic cancers and retards the growth of human tumor xenografts. GSK1838705A does not significantly affect other kinases. GSK1838705A has minimal effects on glucose homeostasis in mice.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable