DCC-2036 (Rebastinib)

Catalog No. A11200

DCC-2036 (Rebastinib)是一种Bcr-Abl抑制剂，作用于Abl1(WT)和Abl1(T315I)，IC50分别为0.8 nM和4 nM，也抑制SRC， LYN， FGR， HCK， KDR， FLT3，和Tie-2，对c-Kit具有低的抑制活性。

Product Citations

Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168

Technical details

Catalog Num	A11200
M. Wt	553.59
Formula	C30H28FN7O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1020172-07-9
Synonyms	DCC2036
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

Biological Activity

Targets

Target	Value
u-Abl1(native)	IC50: 0.75nM
Abl1(H396P)	IC50: 1.4nM
p-Abl1(native)	IC50: 2nM
FLT3	IC50: 2nM
p-Abl1(T315I)	IC50: 4nM
KDR	IC50: 4nM
u-Abl1(T315I)	IC50: 5nM
Tie-2	IC50: 6nM
Lyn	IC50: 29nM
Src	IC50: 34nM
FGR	IC50: 38nM
Hck	IC50: 40nM
PDGFRα	IC50: 70nM
PDGFRβ	IC50: 113nM
c-Kit	IC50: 481nM
AuroraA	IC50: >5μM
CDK2/CyclinD	IC50: >5μM

Solubility *

In vitro (25°C)	DMSO	103 mg/mL (186.05 mM)
	Water	Insoluble
	Ethanol	15 mg/mL (27.09 mM)
In vivo	0.5% CMC+0.25% Tween 80	15 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	18.06 mL	90.32 mL	180.64 mL
0.5 mM	3.61 mL	18.06 mL	36.13 mL
1 mM	1.81 mL	9.03 mL	18.06 mL
5 mM	0.36 mL	1.81 mL	3.61 mL

*The above data is based on the productmolecular weight 553.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.