ChemicalBook > CAS DataBase List > TAK-659 (hydrochloride)

TAK-659 (hydrochloride)

Product Name
TAK-659 (hydrochloride)
CAS No.
1952251-28-3
Chemical Name
TAK-659 (hydrochloride)
Synonyms
CS-2611;TAK-659 HCl;TAK659;TAK 659;TAK-659;TAK-659 (hydrochloride);TAK-659 hydrochloride (Mivavotinib;6-{[(1R,2S)-2-aminocyclohexyl]amino}-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H,2H,3H-pyrrolo[3,4-c]pyridin-3-one hydrochloride;6-(((1R,2S)-2-Aminocyclohexyl)amino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one hydrochloride;Spleen,Inhibitor,Spleen tyrosine kinase,TAK659,Cluster of differentiation antigen 135,inhibit,CLL,related,tyrosine,kinase,FLT3,Fms like tyrosine kinase 3,CD135,TAK 659 hydrochloride,TAK659 hydrochloride,fms,Syk,TAK 659
CBNumber
CB63339718
Molecular Formula
C17H22ClFN6O
Formula Weight
380.85
MOL File
1952251-28-3.mol
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TAK-659 (hydrochloride) Property

storage temp. 
Store at -20°C
solubility 
DMSO : < 1 mg/mL (insoluble or slightly soluble);Water : 2 mg/mL (5.25 mM; ultrasonic and adjust pH to 3 with HCl)
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6988
Product name
TAK-659(hydrochloride)
Purity
99.69%
Packaging
2mg
Price
$90
Updated
2021/12/16
ChemScene
Product number
CS-6988
Product name
TAK-659(hydrochloride)
Purity
99.69%
Packaging
5mg
Price
$140
Updated
2021/12/16
ChemScene
Product number
CS-6988
Product name
TAK-659(hydrochloride)
Purity
99.69%
Packaging
10mg
Price
$190
Updated
2021/12/16
ChemScene
Product number
CS-6988
Product name
TAK-659(hydrochloride)
Purity
99.69%
Packaging
25mg
Price
$390
Updated
2021/12/16
ChemScene
Product number
CS-6988
Product name
TAK-659(hydrochloride)
Purity
99.69%
Packaging
50mg
Price
$590
Updated
2021/12/16
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TAK-659 (hydrochloride) Chemical Properties,Usage,Production

Uses

TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)[1][2][3][4].

in vivo

TAK-659 hydrochloride (100 mg/kg/day; p.o.; daily, for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments[4].
TAK-659 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors[4].
TAK-659 hydrochloride treatment abrogates metastasis of tumor cells into bone marrow[4].

Animal Model:LMP2A/MYC double transgenic mice[4]
Dosage:100 mg/kg/day
Administration:Oral gavage; for 10 days
Result:Inhibited LMP2A-induced tumor cell survival in vivo.

References

[1] Lam B, et al. Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett. 2016 Dec 15;26(24):5947-5950. DOI:10.1016/j.bmcl.2016.10.087
[2] Purroy N, et al. Inhibition of BCR signaling using the Syk inhibitor TAK-659 prevents stroma-mediated signaling in chronic lymphocytic leukemia cells. Oncotarget. 2017 Jan 3;8(1):742-756. DOI:10.18632/oncotarget.13557
[3] Jie Yu, et al. Anti-tumor activity of TAK-659, a dual inhibitor of SYK and FLT-3 kinases, in AML models. Journal of Clinical Oncology 34, no. 15_suppl.
[4] Cen O, et al. Spleen Tyrosine Kinase Inhibitor TAK-659 Prevents Splenomegaly and Tumor Development in a Murine Model of Epstein-Barr Virus-Associated Lymphoma. mSphere. 2018 Aug 22;3(4). DOI:10.1128/mSphereDirect.00378-18

TAK-659 (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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TAK-659 (hydrochloride) Suppliers

Chembest Research Laboratories Limited
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+86-21-20908456
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021-58180499
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sales@BioChemBest.com
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China
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Shanghai Topbiochem Technology Co., Ltd
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021-58170097
Email
info@topbiochem.com
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China
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MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696,15000506266 15000506266
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+86-21-52996696
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China
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
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China
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ShangHai Biochempartner Co.,Ltd
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177-54423994 17754423994
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China
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Suzhou Ran enzyme Biotechnology Co., Ltd.
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Twochem Co.Ltd.
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Guangzhou Tomums Life Science Co., Ltd.
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1952251-28-3, TAK-659 (hydrochloride)Related Search:


  • 6-(((1R,2S)-2-Aminocyclohexyl)amino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one hydrochloride
  • CS-2611
  • TAK659;TAK 659;TAK-659
  • TAK-659 (hydrochloride)
  • TAK-659 HCl
  • 6-{[(1R,2S)-2-aminocyclohexyl]amino}-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H,2H,3H-pyrrolo[3,4-c]pyridin-3-one hydrochloride
  • Spleen,Inhibitor,Spleen tyrosine kinase,TAK659,Cluster of differentiation antigen 135,inhibit,CLL,related,tyrosine,kinase,FLT3,Fms like tyrosine kinase 3,CD135,TAK 659 hydrochloride,TAK659 hydrochloride,fms,Syk,TAK 659
  • TAK-659 hydrochloride (Mivavotinib
  • 1952251-28-3