1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl

BCR-ABL-IN-2 

Cat. No.: HY-18819
Handling Instructions

BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.

For research use only. We do not sell to patients.

BCR-ABL-IN-2 Chemical Structure

BCR-ABL-IN-2 Chemical Structure

CAS No. : 897369-18-5

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  • Biological Activity

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Description

BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.

IC50 & Target[1]

ABL1native

57 nM (IC50)

ABL1T315I

773 nM (IC50)

In Vitro

BCR-ABL-IN-2 (Compound 1) contains a urea moiety to allow a hydrogen bond with the conserved K271-E286 salt bridge of ABL1, a t-butyl moiety to bind into the hydrophobic spine at the third pocket position, and a 2,3-dichlorophenyl ring to stabilize the DFG-phenylalanine F382 in the Type II-out conformation. BCR-ABL-IN-2 exhibits an IC50 of 57 nM for ABL1native and an IC50 of 773 nM for ABL1T315I[1]. Despite ABL, BCR-ABL-IN-2 can also inhibit KDR, BRaf, p38 kinase with IC50s of 1.8 μM, 0.23 μM, 6.3 nM, 43 nM, respectively[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9905 mL 9.9524 mL 19.9049 mL
5 mM 0.3981 mL 1.9905 mL 3.9810 mL
10 mM 0.1990 mL 0.9952 mL 1.9905 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

502.39

Formula

C₂₄H₂₅Cl₂N₅O₃

CAS No.

897369-18-5

SMILES

O=C([[email protected]]1NCC2=C(C=C(N3N=C(C(C)(C)C)C=C3NC(NC4=CC=CC(Cl)=C4Cl)=O)C=C2)C1)O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BCR-ABL-IN-2
Cat. No.:
HY-18819
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BCR-ABL-IN-2

Cat. No.: HY-18819