GSK1838705A
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 401475

CAS#: 1116235-97-2

Description: GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively . GSK1838705A blocks 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 observed at efficacious doses. GSK1838705A also inhibits the anaplastic lymphoma kinase (ALK), which drives the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non-small cell lung cancers. GSK1838705A inhibits ALK, with an IC(50) of 0.5 nmol/L, and causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses. GSK1838705A is therefore a promising antitumor agent for therapeutic use in human cancers. (source: Mol Cancer Ther. 2009 Oct;8(10):2811-20. ).


Price and Availability

Size
Price

5mg
USD 150
50mg
USD 750
500mg
USD 2250
Size
Price

10mg
USD 250
100mg
USD 950
1g
USD 3650
Size
Price

25mg
USD 450
200mg
USD 1450
5g
Ask price

GSK1838705A, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 401475
Name: GSK1838705A
CAS#: 1116235-97-2
Chemical Formula: C27H29FN8O3
Exact Mass: 532.23467
Molecular Weight: 532.57
Elemental Analysis: C, 60.89; H, 5.49; F, 3.57; N, 21.04; O, 9.01


Synonym: GSK1838705A; GSK-1838705A; GSK 1838705A.

IUPAC/Chemical Name: 2-((2-((1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-6-fluoro-N-methylbenzamide

InChi Key: HZTYDQRUAWIZRE-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(NC)C1=C(F)C=CC=C1NC2=C3C(NC=C3)=NC(NC4=CC5=C(C=C4OC)CCN5C(CN(C)C)=O)=N2


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Bao NR, Lu M, Bin FW, Chang ZY, Meng J, Zhou LW, Guo T, Zhao JN. Systematic screen with kinases inhibitors reveals kinases play distinct roles in growth of osteoprogenitor cells. Int J Clin Exp Pathol. 2013 Sep 15;6(10):2082-91. eCollection 2013. PubMed PMID: 24133586; PubMed Central PMCID: PMC3796230.

2: Ardini E, Magnaghi P, Orsini P, Galvani A, Menichincheri M. Anaplastic Lymphoma Kinase: role in specific tumours, and development of small molecule inhibitors for cancer therapy. Cancer Lett. 2010 Dec 28;299(2):81-94. doi: 10.1016/j.canlet.2010.09.001. Epub 2010 Oct 8. Review. PubMed PMID: 20934803.

3: Kelleher FC, McDermott R. The emerging pathogenic and therapeutic importance of the anaplastic lymphoma kinase gene. Eur J Cancer. 2010 Sep;46(13):2357-68. doi: 10.1016/j.ejca.2010.04.006. Epub 2010 May 5. Review. PubMed PMID: 20451371.

4: Sabbatini P, Korenchuk S, Rowand JL, Groy A, Liu Q, Leperi D, Atkins C, Dumble M, Yang J, Anderson K, Kruger RG, Gontarek RR, Maksimchuk KR, Suravajjala S, Lapierre RR, Shotwell JB, Wilson JW, Chamberlain SD, Rabindran SK, Kumar R. 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. doi: 10.1158/1535-7163.MCT-09-0423. PubMed PMID: 19825801.