Rebastinib

SKU: orb1305227

Description

Rebastinib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1020172-07-9
• MW: 553.59
• Purity: 99.84%
• Formula: C₃₀H₂₈FN₇O₃
• SMILES: CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3cc(nn3-c3ccc4ncccc4c3)C(C)(C)C)c(F)c2)ccn1
• Target: Bcr-Abl,FLT,Apoptosis,Src
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.81 mM);Ethanol:13 mg/mL (23.48 mM);DMSO:5.54 mg/mL (10.01 mM)

Bioactivity

• Target IC50:
  Abl-1 (T315I):4 nM|Abl-1 (WT):0.8 nM
• In Vivo:
  DCC-2036 exhibits ant Proliferative activity against Ba/F3 cells expressing either wild-type or mutant BCR-ABL1, with IC50 Values ranging from 2 to 150 nM. It also inhibit the proliferation o the Ph+ cell line K562 IC50 5.5 nM) and effectively induces apoptosis in Ba/F3 and K562 cells expressing BCR-ABL1. Notably, DCC-2036 selectively inhibits BCR-ABL positive cells by significantly suppressing mL cell lines compared to non- mL leukemia cell lines. It demonstrates potent non-ATP-competitive Inhibition against unphosphorylated and phosphorylated ABL1 IC50 0.8/2 nM), unphosphorylated and phosphorylated mutant ABL1T315I IC50 1.4/5 nM), an the activation loop mutant ABL1H396P IC50 4 nM). Additionally, DCC-2036 inhibits SRC family kinases SRC/LYN/FGR/HCK and receptor TKs KDR/FLT3/TIE2 IC50 34/29/38/40/4/2/6 nM).
• In Vitro:
  In a xenograft mouse model bearing Ba/F3-BCR-ABL1T315I leukemia cells, DCC-2036 (100 mg/kg/day, p.o.) significantly inhibits BCR-ABL1 signaling and notably prolong the lifespan o the mice.
• Cell Research:
  Ba/F3 cells or Primary Ph+ leukemia cells are plated in triplicate in 96-well plates containing test compounds. After 72 hours, viable cells are quantified by Resazurin or MTT assay. Cells are diluted in medium to be added to each well of a 96-well tissue culture-treated plate. All cells are incubated overnight and maintained in a humidified atmosphere at 37℃nd 5% CO2. Cells are treate the following day. Serum-free medium is used during treatment with DCC-2036. MTT is used to asses the viability of cells following treatment. Aliquots of 20 mL of stock MTT solution are added to each well containing 200 mL of medium (10% final solution) and incubated wit the cells for 2 hours. Following incubatio the medium is removed and 200 mL of dimethylsulfoxide added to solubiliz the formazan crystals the absorbance is read o the plate reader at 550 and 690 nM. A subtraction analysis o the dual wavelength is performed (D550 to D690) to increase accuracy o the measuremen(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Cluster of differentiation antigen 135, CD135, DCC 2036, DCC-2036, DCC2036, Abl1, Apoptosis, Bcr-Abl, BcrAbl, inhibit, p-Abl1 (native), p-Abl1 (T315I), Inhibitor, FLT3, Fms like tyrosine kinase 3, Rebastinib, Src, u-Abl1 (native)

Compound Identifiers

PubChem CID

25066467