Bafetinib

ArtNr	S1369-200
Hersteller	Selleckchem
CAS-Nr.	859212-16-1
Menge	200 mg
Quantity options	10 mg 100 mg 10 mM/1 mL 1 g 200 mg 25 mg 5 mg 50 mg
Kategorie	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Colorectal Cancer Heart & Blood Cancer Testicular & Prostate Cancer
Typ	Inhibitors
Specific against	other
Smiles	CC1=C(C=C(C=C1)NC(=O)C2=CC(=C(C=C2)CN3CCC(C3)N(C)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CN=C5
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	INNO-406,NS-187
Similar products	Bafetinib
Lieferbar
Manufacturer - Targets	LYN, BCR
Storage Conditions	2 years -80 in solvent
Molecular Weight	576, 62
Administration	Administered via p.o.
Animal Models	KU812 xenograft is established by subcutaneous injection of KU812 cells into the right flank of Balb/c-nu/nu female mice.
Cell lines	K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells
Clinical Trials	Bafetinib is currently in Phase II clinical trials in patients with hormone refractory prostate cancer.
Concentrations	0-10 uM
Dosages	<=20 mg/kg/day
Formulation	Bafetinib is dissolved in 0.5% methylcellulose.
IC50	5.8 nM, 5.8 nM, 5.8 nM, 5.8 nM, 5.8 nM, 5.8 nM
In vitro	Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells, respectively. Bafetinib suppresses the growth of the Bcr-Abl-positive cell lines including K562, KU812, and BaF3/wt cells potently without effects on the proliferation of the Bcr-Abl-negative U937 cell line. Moreover, Bafetinib exhibits a dose-dependent antiproliferative effect against Bcr-Abl point mutant cell lines, such as BaF3/E255K cells. [1] In Bcr-Abl+ leukemia cell lines, Bafetinib induces both caspase-mediated and caspase-independent cell death by blocking the phosphorylation of Bcr-Abl. [2]
In vivo	In Bcr-Ablâ€“positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. [1] In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and cyclosporine A (CsA) (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone. [3]
Incubation Time	72 hours
Kinase Assay	Kinase assay, Bcr-Abl kinase assays are performed in 25 uL of reaction mixture containing 250 uM peptide substrate, 740 Bq/uL [gamma-33P]ATP, and 20 uM cold adenosine triphosphate (ATP) by using the SignaTECT protein tyrosine kinase assay system. Each Bcr-Abl kinase is used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn are carried out with an enzyme-linked immunosorbent assay (ELISA) kit. The inhibitory effects of NS-187 against 79 tyrosine kinases are tested with KinaseProfiler.
Method	K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells are plated at 1, 103 in 96-well plates, whereas KU812 and U937 cells are plated at 5, 103 in 96-well plates. Cells are incubated with serial dilutions of Bafetinib for 3 days. Cell proliferation is measured by MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, Nacalai Tesque) assay, and the 50% inhibitory concentration (IC50) values are calculated by fitting the data to a logistic curve.
Information	Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.
Chemical Name	(S)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-N-(4-methyl-3-(4-(pyrimidin-5-yl)pyrimidin-2-ylamino)phenyl)-3-(trifluoromethyl)benzamide
Features	Dual Bcr-Abl/Lyn inhibitor

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