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Rebastinib

Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.

Product Specifications

CAS Number

[1020172-07-9]

Product Name Alternative

DCC-2036

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Bcr-Abl; FLT3; Src

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/DCC-2036.html

Concentration

10mM

Purity

99.91

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

CC(C)(C)C1=NN(C(NC(NC2=C(F)C=C(OC3=CC(C(NC)=O)=NC=C3)C=C2)=O)=C1)C4=CC=C5C(C=CC=N5)=C4

Molecular Formula

C30H28FN7O3

Molecular Weight

553.59

Precautions

H302, H315, H319, H335

References & Citations

[1]Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011, 19 (4), 556-568.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Available Sizes

Curated Selection

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