Bafetinib (INNO-406)

Catalog No.S1369 Synonyms: NS-187

Bafetinib (INNO-406) Chemical Structure

Molecular Weight(MW): 576.62

Bafetinib (INNO-406) 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. Phase 2.

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Cited by 5 Publications

1 Customer Review

  • (A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.

    Scientific Reports, 2016, 6:25694.. Bafetinib (INNO-406) purchased from Selleck.

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Biological Activity

Description Bafetinib (INNO-406) 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. Phase 2.
Features Dual Bcr-Abl/Lyn inhibitor.
Targets
Abl [1]
(Cell-free assay)		 Lyn [1]
(Cell-free assay)
5.8 nM 19 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-Abl–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]

Protocol

Kinase Assay:[1]
+ Expand

Kinase assay :

Bcr-Abl kinase assays are performed in 25 μL of reaction mixture containing 250 μM peptide substrate, 740 Bq/μL [γ-33P]ATP, and 20 μM 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.
Cell Research:[1]
+ Expand
  • Cell lines: K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells
  • Concentrations: 0-10 μM
  • Incubation Time: 72 hours
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: KU812 xenograft is established by subcutaneous injection of KU812 cells into the right flank of Balb/c-nu/nu female mice.
  • Formulation: Bafetinib is dissolved in 0.5% methylcellulose.
  • Dosages: ≤20 mg/kg/day
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (173.42 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 576.62
Formula

C30H31F3N8O
CAS No. 859212-16-1
Storage powder
in solvent
Synonyms NS-187

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01234740 Completed Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor|Tumors Metastatic to Brain|Adult Anaplastic Oligoastrocytoma City of Hope Medical Center|National Cancer Institute (NCI) December 2010 Phase 1
NCT01234740 Completed Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor|Tumors Metastatic to Brain|Adult Anaplastic Oligoastrocytoma City of Hope Medical Center|National Cancer Institute (NCI) December 2010 Phase 1
NCT01215799 Completed Hormone Refractory Prostate Cancer CytRx August 2010 Phase 2
NCT01215799 Completed Hormone Refractory Prostate Cancer CytRx August 2010 Phase 2
NCT01144260 Completed B-Cell Chronic Lymphocytic Leukemia CytRx June 2010 Phase 2
NCT01144260 Completed B-Cell Chronic Lymphocytic Leukemia CytRx June 2010 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    Can you suggest the route of in vivo administration for S1369?

  • Answer:

    S1369 in 0.5% methylcellulose+0.2% Tween 80 at 30mg/ml is a suspension, and it is fine for oral gavage. If you dissolved the compound in 0.5% methyl cellulose and got a suspension, it is fine. And 0.2% Tween 80 can help the suspension dissolving more homogeneous.

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Bcr-Abl Signaling Pathway Map

Bcr-Abl Inhibitors with Unique Features

  • Selective Bcr-Abl Inhibitor

    Nilotinib (AMN-107) : Bcr-Abl-selective, IC50<30 nM.

  • Most Potent Bcr-Abl Inhibitor

    GZD824 : Bcr-Abl(WT), IC50=0.34 nM; Bcr-Abl(T315I), IC50=0.68 nM.

  • FDA-approved Bcr-Abl Inhibitor

    Dasatinib : Approved by FDA for CML and Ph+ ALL.

  • Newest Bcr-Abl Inhibitor

    GZD824 : Orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID