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Rebastinib - CAS 1020172-07-9

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Catalog Number	Size	Price	Stock	Quantity
BP-300144	50 mg	$299	In stock

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Rebastinib is an orally bioactive inhibitor of Bcr-Abl that binds to and inhibits Bcr-Abl fusion oncoprotein. Rebastinib changes the conformation of the folded protein to disallow ligand-dependent and ligand-independent activation. It also exhibits inhibitory activity at SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2.

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Molecular Formula

C30H28FN7O3

Molecular Weight

553.598

Rebastinib

- Specification
  - Purity
    
    ≥98%
    
    Appearance
    
    Off-White Solid
    
    Application
    
    Antineoplastic Agents
    
    IUPAC Name
    
    4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
    
    Synonyms
    
    DCC2036; DCC-2036; DCC 2036; Rebastinib. 4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
- Properties
  - Melting Point
    
    >181°C (dec.)
    
    InChI Key
    
    WVXNSAVVKYZVOE-UHFFFAOYSA-N
    
    InChI
    
    InChI=1S/C30H28FN7O3/c1-30(2,3)26-17-27(38(37-26)19-7-9-23-18(14-19)6-5-12-33-23)36-29(40)35-24-10-8-20(15-22(24)31)41-21-11-13-34-25(16-21)28(39)32-4/h5-17H,1-4H3,(H,32,39)(H2,35,36,40)
    
    Canonical SMILES
    
    CC(C)(C)C1=NN(C(=C1)NC(=O)NC2=C(C=C(C=C2)OC3=CC(=NC=C3)C(=O)NC)F)C4=CC5=C(C=C4)N=CC=C5
- Reference Reading
  - 1.BCR-ABL1 compound mutations combining key kinase domain positions confer clinical resistance to ponatinib in Ph chromosome-positive leukemia.
    Zabriskie MS1, Eide CA2, Tantravahi SK3, Vellore NA4, Estrada J1, Nicolini FE5, Khoury HJ6, Larson RA7, Konopleva M8, Cortes JE8, Kantarjian H8, Jabbour EJ8, Kornblau SM8, Lipton JH9, Rea D10, Stenke L11, Barbany G12, Lange T13, Hernández-Boluda JC14, Oss Cancer Cell. 2014 Sep 8;26(3):428-42. doi: 10.1016/j.ccr.2014.07.006. Epub 2014 Aug 14.
    Ponatinib is the only currently approved tyrosine kinase inhibitor (TKI) that suppresses all BCR-ABL1 single mutants in Philadelphia chromosome-positive (Ph(+)) leukemia, including the recalcitrant BCR-ABL1(T315I) mutant. However, emergence of compound mutations in a BCR-ABL1 allele may confer ponatinib resistance. We found that clinically reported BCR-ABL1 compound mutants center on 12 key positions and confer varying resistance to imatinib, nilotinib, dasatinib, ponatinib, rebastinib, and bosutinib. T315I-inclusive compound mutants confer high-level resistance to TKIs, including ponatinib. In vitro resistance profiling was predictive of treatment outcomes in Ph(+) leukemia patients. Structural explanations for compound mutation-based resistance were obtained through molecular dynamics simulations. Our findings demonstrate that BCR-ABL1 compound mutants confer different levels of TKI resistance, necessitating rational treatment selection to optimize clinical outcome.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 1.8064 mL 9.0320 mL 18.0639 mL
    
    5 mM 0.3613 mL 1.8064 mL 3.6128 mL
    
    10 mM 0.1806 mL 0.9032 mL 1.8064 mL
    
    50 mM 0.0361 mL 0.1806 mL 0.3613 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	1.8064 mL	9.0320 mL	18.0639 mL
5 mM	0.3613 mL	1.8064 mL	3.6128 mL
10 mM	0.1806 mL	0.9032 mL	1.8064 mL
50 mM	0.0361 mL	0.1806 mL	0.3613 mL

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