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DCC-2036

DCC-2036

品 牌 MCE
C A S 号 1020172-07-9
货 号 HY-13024
规 格 5mg
价 格(元) 1581.00
咨询优惠价
货号 规格 价格
HY-13024 5mg 1581.00
HY-13024 10mg 2418.00
HY-13024 50mg 7068.00

产品说明


DCC-2036(Rebastinib)是Bcr-Abl抑制剂,对Abl1(WT)和Abl1(T315I)的IC50分别为0.8 nM和4 nM,



DCC-2036的生物活性


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].

化学信息


分子量 553.59 储存条件 参考CoA中推荐的条件进行储存。
分子式 C₃₀H₂₈FN₇O₃
CAS号 1020172-07-9
溶剂/溶解度 10 mM in DMSO

相关文献


[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-ABLT315I and exhibits a narrow resistance profile. Cancer Res. 2011, 71(9), 3189-3195.