DCC-2036 Inhibitor CAS No. 1020172-07-9

Cat. No.	Name	Size	Price
KI0530	DCC-2036	10 mg	$512
	DCC-2036	50 mg	$1552
	DCC-2036	100 mg	$2672
	DCC-2036	200 mg	$3952

Chemical Characteristic

Product Name	DCC-2036
Synonyms	Rebastinib
CAS No.	1020172-07-9
Molecular Weight	553.59
Formula	C₃₀H₂₈FN₇O₃
Chemical Name	N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea
Smiles	N(C(=O)Nc1c(cc(cc1)Oc1cc(ncc1)C(=O)NC)F)c1n(nc(c1)C(C)(C)C)c1cc2cccnc2cc1
Chemical Structure

Biological activities

DCC-2036 is a conformational control inhibitor of ABL1 and ABL1(T315I). DCC-2036 inhibits ABL1 and ABLT1^315I with IC50 values of 0.8 and 4 nM, respectively. DCC-2036 inhibits purified native ABL1 in unphosphorylated (u-ABL1^native) and phosphorylated (p-ABL1^native) forms with IC50 values of 0.8 and 2 nM, respectively. DCC-2036 inhibits purified native ABL1 in unphosphorylated (u-ABL1^native) and phosphorylated (p-ABL1^native) forms with IC50 values of 0.8 and 2 nM, respectively. DCC-2036 inhibits unphosphorylated and phosphorylated gatekeeper mutant ABLT1^315I, and the activation loop mutant ABL1^H396P in a non-ATP-competitive manner with IC50 values of 1.4, 5, and 4 nM, respectively. In addition to ABL1, DCC-2036 also inhibits the SRC family kinases SRC, LYN, FGR, and HCK, and the receptor TKs KDR, FLT3, and TIE2 with IC50 of 34, 29, 38, 40, 4, 2 and 6 nM, respectively. In vitro, DCC-2036 inhibits cellular proliferation of Ba/F3 cells expressing native or mutant BCR-ABL1.^[1] In chronic myeloid leukemia (CML) cells harboring BCR-ABL or BCR-ABLT^315I to DCC-2036 inhibits colony formation and reduces phosphorylation of the direct BCR-ABL target CrkL.^[2] In a mouse Ba/F3 cell allograft model, DCC-2036 treatment (100 mg/kg) inhibits mutant BCR-ABLT1^315I signaling and prolongs survival.^[1]

Protocols

In vivo: DCC-2036 is dissolved in 0.5% CMC/1% Tween-80.^[1]

References

[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. [2] Eide CA, et al. The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT^315I and exhibits a narrow resistance profile. Cancer Res. 2011, 71(9): 3189-3195.

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