Bafetinib (INNO-406)

For research use only.

Catalog No.S1369 Synonyms: NS-187

16 publications

Bafetinib (INNO-406) Chemical Structure

CAS No. 859212-16-1

Bafetinib (INNO-406, NS-187) 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.

Selleck's Bafetinib (INNO-406) has been cited by 16 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.

Purity & Quality Control

Choose Selective Bcr-Abl Inhibitors

Biological Activity

Description Bafetinib (INNO-406, NS-187) 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • Animal Models: KU812 xenograft is established by subcutaneous injection of KU812 cells into the right flank of Balb/c-nu/nu female mice.
  • 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
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00352677 Completed Drug: INNO-406 Chronic Myeloid Leukemia|Acute Lymphocytic Leukemia CytRx July 2006 Phase 1

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

selleck catalog

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.

Related Bcr-Abl Products

  • PX-478 2HCl New

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.

  • Defactinib (VS-6063) New

    Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

  • SU6656 New

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • Imatinib (STI571) Mesylate

    Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.

  • Ponatinib (AP24534)

    Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.

  • Nilotinib (AMN-107)

    Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.

    Features:A selective inhibitor of native and mutant Bcr-Abl.

  • Degrasyn (WP1130)

    Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.

    Features:WP1130 has an advantage over imatinib mesylate in that its activity is not inhibited by a variety of Abl kinase mutations, including T315I.

  • Rebastinib (DCC-2036)

    Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.

    Features:A conformational control inhibitor of Abl1 and T315I Abl1.

  • Olverembatinib dimesylate (HQP1351)

    Olverembatinib dimesylate (HQP1351, GZD824) is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

Tags: buy Bafetinib (INNO-406) | Bafetinib (INNO-406) supplier | purchase Bafetinib (INNO-406) | Bafetinib (INNO-406) cost | Bafetinib (INNO-406) manufacturer | order Bafetinib (INNO-406) | Bafetinib (INNO-406) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID