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GSK1838705A - 10mM in DMSO, high purity , CAS No.1116235-97-2(DMSO), Inhibitor of ALK receptor tyrosine kinase;Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of ribosomal protein S6 kinase A1

COA COA
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Item Number
G408364
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G408364-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$321.90
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ALK Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms 2-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-6-fluoro-N-methylbenzamide
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of ALK receptor tyrosine kinase;Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of ribosomal protein S6 kinase A1
Product Description

Information

GSK1838705A GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.
In vitro

GSK1838705A potently and ATP-competitively inhibits IGF-1R and IR with appKi values of 0.7 nM and 1.1 nM, respectively.In cells, GSK1838705A potently inhibits ligand-induced phosphorylation of IGF-1R and IR with IC50 of 85 nM and 79 nM, respectively. GSK1838705A shows the significant anti-proliferative effect in a panel of cell lines derived from solid and hematologic tumors such as L-82, SUP-M2, SK-ES and MCF-7 cells with EC50 of 24 nM, 28 nM, 141 nM and 203 nM, respectively. GSK1838705A shows an accumulation of MCF-7 and NCl-H929 cells predominantly in G1 (2N) phase of the cell cycle. GSK1838705A also inhibits ALK with Ki of 0.35 nM and supresses the proliferation of nucleophosmin (NPM)-ALK fusion cells with EC50 of 24-88 nM. GSK1838705A potently inhibits NPM-ALK phosphorylation in Karpas-299 and SR-786 cells, while has modest effect on STAT3 phosphorylation.

In vivo

In NIH-3T3/LISN tumor-bearing mice, oral treatment of GSK1838705A (60 mg/kg) cause tumor growth inhibition by 77%, without significant weight loss. In COLO 205 tumor-bearing mice, inhibition of tumor growth by GSK1838705A (30 mg/kg) is 80%. Besides, the antitumor efficacy of GSK1838705A is also observed in mice bearing HT29 xenograft or BxPC3 xenograft. In mice, GSK1838705A (60 mg/kg) leads to a transient 2-fold increase in blood glucose levels by inhibiting IR signaling. GSK1838705A (60 mg/kg) inhibits the growth of established Karpas-299 xenografts with 93% tumor growth inhibition, with no effect on weights of the rats.
Cell Data

cell lines：HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, HepG2, MCF-7, MDA-MB-468 and BT-474 cell lines

Concentrations：0 to 10 μM

Incubation Time：72 hours

Powder Purity:≥96%

Product Properties

ALogP 3.508
hba_count 5
HBD Count 4
Rotatable Bond 8

Associated Targets(Human)

ROS1 Tclin Proto-oncogene tyrosine-protein kinase ROS (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FER Tclin Tyrosine-protein kinase Fer (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
IGF1R Tclin Insulin-like growth factor 1 receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha-1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
LTK Tclin Leukocyte tyrosine kinase receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ALK Tclin ALK tyrosine kinase receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CLK1 Tchem Dual specificity protein kinase CLK1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CLK2 Tchem Dual specificity protein kinase CLK2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
INSRR Tchem Insulin receptor-related protein (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
INSR Tclin Insulin receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MYLK Tchem Myosin light chain kinase, smooth muscle (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles CNC(=O)C1=C(F)C=CC=C1NC2=C3C=C[NH]C3=NC(=N2)NC4=C(OC)C=C5CCN(C(=O)CN(C)C)C5=C4
Molecular Weight 532.57
Reaxy-Rn 18983141
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18983141&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 107
DMSO(mM) Max Solubility 200.91
Water(mg / mL) Max Solubility <1

Solution Calculators

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