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936091-14-4,MFCD15528085
Catalog No.:AA00GU47

936091-14-4 | TG 101209

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98+%
in stock  
$14.00   $10.00
- +
10mg
98+%
in stock  
$48.00   $34.00
- +
25mg
98+%
in stock  
$81.00   $57.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00GU47
Chemical Name:
TG 101209
CAS Number:
936091-14-4
Molecular Formula:
C26H35N7O2S
Molecular Weight:
509.6668
MDL Number:
MFCD15528085
SMILES:
CN1CCN(CC1)c1ccc(cc1)Nc1ncc(c(n1)Nc1cccc(c1)S(=O)(=O)NC(C)(C)C)C
Properties
Computed Properties
 
Complexity:
783  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
36  
Hydrogen Bond Acceptor Count:
9  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
8  
XLogP3:
4.2  

Downstream Synthesis Route
308283-47-8    936092-52-3   
TG101209 

[1]Patent:WO2007/53452,2007,A1.Locationinpatent:Page/Pagecolumn108-109

[1]CurrentPatentAssignee:HANDANWINCONDRUGINTERMEDIATERESDEV;SHANGHAIWINCONCHEMRD-CN103242240,2016,BLocationinpatent:Paragraph0091-0095

[1]CurrentPatentAssignee:HANDANWINCONDRUGINTERMEDIATERESDEV;SHANGHAIWINCONCHEMRD-CN103242240,2016,BLocationinpatent:Paragraph0081-0085

936092-53-4   
TG101209 

[1]CurrentPatentAssignee:SHANGHAIWINCONCHEMRD;HANDANWINCONDRUGINTERMEDIATERESDEV-CN103242240,2016,B

[2]CurrentPatentAssignee:SHANGHAIWINCONCHEMRD;HANDANWINCONDRUGINTERMEDIATERESDEV-CN103242240,2016,B

[3]CurrentPatentAssignee:SHANGHAIWINCONCHEMRD;HANDANWINCONDRUGINTERMEDIATERESDEV-CN103242240,2016,B

Literature

Title: The HDAC inhibitor Givinostat modulates the hematopoietic transcription factors NFE2 and C-MYB in JAK2(V617F) myeloproliferative neoplasm cells.

Journal: Experimental hematology 20120801

Title: Heat shock protein 90 inhibitor is synergistic with JAK2 inhibitor and overcomes resistance to JAK2-TKI in human myeloproliferative neoplasm cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20111201

Title: Janus kinase 2 regulates Bcr-Abl signaling in chronic myeloid leukemia.

Journal: Leukemia 20110301

Title: TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

Journal: American journal of hematology 20100901

Title: Prolactin-induced Jak2 phosphorylation of RUSH: a key element in Jak/RUSH signaling.

Journal: Molecular and cellular endocrinology 20100830

Title: Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells.

Journal: Blood 20091203

Title: TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations.

Journal: Leukemia 20070801

Title: Pardanani A, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007 Aug;21(8):1658-68.

Title: Ma AC, et al. A novel zebrafish jak2a(V581F) model shared features of human JAK2(V617F) polycythemia vera. Exp Hematol. 2009 Dec;37(12):1379-1386.e4.

Title: Sun Y, et al. Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. J Thorac Oncol. 2011 Apr;6(4):699-706

Title: Cuesta-Dominguez A, et al. Transforming and tumorigenic activity of JAK2 by fusion to BCR: molecular mechanisms of action of a novel BCR-JAK2 tyrosine-kinase. PLoS One. 2012;7(2):e3245

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SDS
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