1. Protein Tyrosine Kinase/RTK
  2. ALK
    IGF-1R
    Insulin Receptor

GSK1838705A 

Cat. No.: HY-13020 Purity: 98.99%
Data Sheet SDS Handling Instructions

GSK1838705A is a potent small-molecule IGF-IR, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively.

For research use only. We do not sell to patients.
GSK1838705A Chemical Structure

GSK1838705A Chemical Structure

CAS No. : 1116235-97-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $176 In-stock
5 mg $150 In-stock
10 mg $250 In-stock
50 mg $750 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK1838705A is a potent small-molecule IGF-1R, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively. IC50 value: 2.0/1.6/0.5 nM ( IGF-1R/InsR/ALK) Target: IGF-1R/InsR/ALK GSK1838705A prevents the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing’s sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were obtained at efficacious doses. A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg led to 35% and 65% prevention of IGF-IR phosphorylation, respectively, whereas doses ≥1 mg/kg led to complete inhibition of ligand-induced IGF-IR phosphorylation. Meanwhile, at a dose of 30 mg/kg, prevention was lasted for ?24 hours after compound injection. GSK1838705A also suppresses the anaplastic lymphoma kinase (ALK), which mediates the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non–small cell lung cancers. Due to its inhibition of ALK, GSK1838705A gives rise to complete regression of ALK-dependent tumors in vivo at well-tolerated doses.

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.8777 mL 9.3884 mL 18.7769 mL
5 mM 0.3755 mL 1.8777 mL 3.7554 mL
10 mM 0.1878 mL 0.9388 mL 1.8777 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

532.57

Formula

C₂₇H₂₉FN₈O₃

CAS No.

1116235-97-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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GSK1838705A
Cat. No.:
HY-13020
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