中文名：Rebastinib (DCC-2036)

英文名：Rebastinib (DCC-2036)

純度：Moligand?，10mM in DMSO

貨號(hào)：R408600

Cas號(hào)：1020172-07-9

存儲(chǔ)溫度：-80℃儲(chǔ)存

運(yùn)輸條件：特低溫運(yùn)輸

產(chǎn)品介紹：

Information

Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor forAbl1(WT)and Abl1(T315I) withIC50of 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. Phase 1.
In?vitro

DCC-2036 shows the potent inhibitory activities against purified native Abl1 in unphosphorylated (u-Abl1^native) and phosphorylated (p-Abl1^native) forms, unphosphorylated and phosphorylated gatekeeper mutant Abl1^T315I, and the activation loop mutant Abl1^H396P 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. DCC-2036 shows the anti-proliferative activities against Ba/F3 cells expressing native or mutant Bcr-Abl1 with IC50 ranging from 2 nM to 150 nM. In addition, DCC-2036 also inhibits proliferation of the Ph⁺ cell line K562 (IC50 5.5 nM), and induces apoptosis in both Bcr-Abl1-expressing Ba/F3 and K562 cells potently. 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.

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.
Cell?Data

cell?lines：

Concentrations：0-10 μM

Incubation?Time：72 hours

Powder?Purity:≥99%

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