CAS No. : 1020172-07-9

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000144
Molecular Formula:C30H28FN7O3
Molecular Weight:553.6
IC50:0.8/4 nM (Abl1 wt/Abl1 T315I) [1]
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Appearance:White to off-white solid powder
Purity: > 98%
Cat No:I000144
Cas No:1020172-07-9

DCC-2036(Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit.
IC50 value: 0.8/4 nM (Abl1 wt/Abl1 T315I) [1]
Target: Abl
in vitro: DCC-2036 shows the potent inhibitory activities against purified native Abl1 in unphosphorylated (u-Abl1native) and phosphorylated (p-Abl1native) forms, unphosphorylated and phosphorylated gatekeeper mutant Abl1T315I, and the activation loop mutant Abl1H396P in a non-ATP-competitive manner with IC50 of 0.8 nM, 2 nM, 1.4 nM, 5 nM, and 4 nM, respectively. Moreover, 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 nM, 29 nM, 38 nM, 40 nM, 4 nM, 2 nM and 6 nM, respectively [1]. A recent study shows that DCC-2036 shows the selectivity for growth inhibition of Bcr-Abl-positive cells by its marked inhibition of CML cell lines compared to non-CML leukemia lines [2].
in vivo: In a mouse allograft model bearing Ba/F3-Bcr-Abl1T315I leukemia cells, DCC-2036 treatment by oral gavage at 100 mg/kg once daily effectively inhibits Bcr-Abl1 signaling and significantly prolongs mouse survival [1].

1:Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia. Cortes J, Talpaz M, Smith HP, Snyder DS, Khoury J, Bhalla KN, Pinilla-Ibarz J, Larson R, Mitchell D, Wise SC, Rutkoski TJ, Smith BD, Flynn DL, Kantarjian HM, Rosen O, Van Etten RA.Haematologica. 2017 Mar;102(3):519-528. doi: 10.3324/haematol.2016.152710. Epub 2016 Dec 7. PMID: 27927766 Free Article
2:The conformational control inhibitor of tyrosine kinases DCC-2036 is effective for imatinib-resistant cells expressing T674I FIP1L1-PDGFRα. Shen Y, Shi X, Pan J.PLoS One. 2013 Aug 29;8(8):e73059. doi: 10.1371/journal.pone.0073059. eCollection 2013. PMID: 24009732 Free PMC Article
3:The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile. Eide CA, Adrian LT, Tyner JW, Mac Partlin M, Anderson DJ, Wise SC, Smith BD, Petillo PA, Flynn DL, Deininger MW, O/'Hare T, Druker BJ.Cancer Res. 2011 May 1;71(9):3189-95. doi: 10.1158/0008-5472.CAN-10-3224. Epub 2011 Apr 19. PMID: 21505103 Free PMC Article
4:Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Chan WW, Wise SC, Kaufman MD, Ahn YM, Ensinger CL, Haack T, Hood MM, Jones J, Lord JW, Lu WP, Miller D, Patt WC, Smith BD, Petillo PA, Rutkoski TJ, Telikepalli H, Vogeti L, Yao T, Chun L, Clark R, Evangelista P, Gavrilescu LC, Lazarides K, Zaleskas VM, Stewart LJ, Van Etten RA, Flynn DL.Cancer Cell. 2011 Apr 12;19(4):556-68. doi: 10.1016/j.ccr.2011.03.003. PMID: 21481795 Free PMC Article
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