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Chemical Structure| 1952251-28-3 Chemical Structure| 1952251-28-3

Structure of TAK-659 HCl
CAS No.: 1952251-28-3

Chemical Structure| 1952251-28-3

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TAK-659 HCl is a selective inhibitor of spleen tyrosine kinase (Syk) with IC50 of 3.2 nM.

Synonyms: TAK-659; TAK-659 hydrochloride; Mivavotinib monohydrochloride

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of TAK-659 HCl

CAS No. :1952251-28-3
Formula : C17H22ClFN6O
M.W : 380.85
SMILES Code : O=C1NCC2=C1C(C3=CN(C)N=C3)=NC(N[C@H]4[C@@H](N)CCCC4)=C2F.[H]Cl
Synonyms :
TAK-659; TAK-659 hydrochloride; Mivavotinib monohydrochloride
English Name :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
MDL No. :MFCD31544322
InChI Key :PTCFBXMEFRIEGV-ZVWHLABXSA-N
Pubchem ID :129626432

Safety of TAK-659 HCl

Related Pathways of TAK-659 HCl

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • FLT3

    FLT3, IC50:4.6 nM

  • Syk

    Syk, IC50:3.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MYC cells 1.66 μM 24 hours Inhibited pSYK mSphere. 2018 Aug 22;3(4):e00378-18.
LMP2A/MYC cells 63 nM 24 hours Totally abrogated pSYK mSphere. 2018 Aug 22;3(4):e00378-18.
MYC cells 5 μM 1 hour Totally inhibited baseline pSYK mSphere. 2018 Aug 22;3(4):e00378-18.
LMP2A/MYC cells 5 μM 1 hour Totally inhibited baseline pSYK mSphere. 2018 Aug 22;3(4):e00378-18.
Primary AML cells 0.05 µM 7 days Evaluate the antiproliferative effect of TAK-659 on AML cells, showing significantly higher antiproliferative effects in FLT3 mutated patients. Int J Mol Sci. 2022 Nov 25;23(23):14706.
Primary AML cells 0.5 µM 7 days Evaluate the antiproliferative effect of TAK-659 on AML cells, showing significantly higher antiproliferative effects in FLT3 mutated patients. Int J Mol Sci. 2022 Nov 25;23(23):14706.
Primary AML cells 0.05 µM 7 days Evaluate the antiproliferative effect of TAK-659 on AML cells, showing strong antiproliferative effects in all seven patient samples tested. Int J Mol Sci. 2022 Nov 25;23(23):14706.
Primary AML cells 0.5 µM 7 days Evaluate the antiproliferative effect of TAK-659 on AML cells, showing strong antiproliferative effects in all seven patient samples tested. Int J Mol Sci. 2022 Nov 25;23(23):14706.
Jurkat T cells 0.1 μM 1 hour TAK-659 did not affect anti-CD3-induced TCR signaling, including phosphorylation of ZAP-70Tyr319, ZAP-70Tyr493, Itk, Akt, and ERK1/2. Oncotarget. 2017 Jan 3;8(1):742-756.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice LMP2A/MYC transgenic mice Oral gavage 100 mg/kg Daily for 10 days Totally abrogated splenomegaly and tumor development mSphere. 2018 Aug 22;3(4):e00378-18.
NSG mice Pediatric ALL patient-derived xenograft models Oral 60 mg/kg Once daily for 21 days To evaluate the in vivo efficacy of TAK-659 against pediatric ALL PDXs. Results showed that TAK-659 significantly prolonged the time to event in 6 out of 8 PDXs tested, but only one PDX achieved an objective response. Pediatr Blood Cancer. 2023 Jun 20:e30503

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.13mL

2.63mL

1.31mL

26.26mL

5.25mL

2.63mL

References

 

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