Product Name :
TAK-659 hydrochloride
Description:
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).
CAS:
1952251-28-3
Molecular Weight:
380.85
Formula:
C17H22ClFN6O
Chemical Name:
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
Smiles :
Cl.CN1C=C(C=N1)C1=NC(N[C@@H]2CCCC[C@@H]2N)=C(F)C2CNC(=O)C1=2
InChiKey:
PTCFBXMEFRIEGV-ZVWHLABXSA-N
InChi :
InChI=1S/C17H21FN6O.ClH/c1-24-8-9(6-21-24)15-13-10(7-20-17(13)25)14(18)16(23-15)22-12-5-3-2-4-11(12)19;/h6,8,11-12H,2-5,7,19H2,1H3,(H,20,25)(H,22,23);1H/t11-,12+;/m0./s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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).|Product information|CAS Number: 1952251-28-3|Molecular Weight: 380.85|Formula: C17H22ClFN6O|Chemical Name: 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|Smiles: Cl.CN1C=C(C=N1)C1=NC(N[C@@H]2CCCC[C@@H]2N)=C(F)C2CNC(=O)C1=2|InChiKey: PTCFBXMEFRIEGV-ZVWHLABXSA-N|InChi: InChI=1S/C17H21FN6O.ClH/c1-24-8-9(6-21-24)15-13-10(7-20-17(13)25)14(18)16(23-15)22-12-5-3-2-4-11(12)19;/h6,8,11-12H,2-5,7,19H2,1H3,(H,20,25)(H,22,23);1H/t11-,12+;/m0./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Mecillinam Purity |Shelf Life: ≥12 months if stored properly.7-Amino-4-methylcoumarin MedChemExpress |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:32970971 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|TAK-659 hydrochloride inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines. TAK-659 hydrochloride (5 µM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment. TAK-659 hydrochloride (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells.|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. TAK-659 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors. TAK-659 hydrochloride treatment abrogates metastasis of tumor cells into bone marrow.|Products are for research use only. Not for human use.|
