DCC-2036 | Bcr-Abl inhibitor | Probechem Biochemicals

Chemical Structure : DCC-2036

CAS No.: 1020172-07-9

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DCC-2036 (Rebastinib;DCC 2036;DCC2036)

货号: PC-43334Not For Human Use, Lab Use Only.

DCC-2036 (Rebastinib) is a highly potent, non-ATP-competitive BCR-ABL1 inhibitor with IC50 of 0.8 and 4 nM for native ABL1 and gatekeeper mutant ABL1 T315I, respectively.

规格	价格	库存
2 mg (Free Sample)	￥280	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥3280	In stock
100 mg		Get quote

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生物&药学活性

DCC-2036 (Rebastinib) is a highly potent, non-ATP-competitive BCR-ABL1 inhibitor with IC50 of 0.8 and 4 nM for native ABL1 and gatekeeper mutant ABL1 T315I, respectively.
DCC-2036 also inhibits the SRC family kinases SRC, LYN, FGR, and HCK, and the receptor TKs KDR, FLT3, and TIE2 (IC50s=2-40 nM), but spares c-KIT (IC50=480 nM).
DCC-2036 potently inhibits unphosphorylated and phosphorylated of ABL1 native with IC50 of 0.75 and 2 nM, potently inhibits unphosphorylated and phosphorylated of ABL1 T315I with IC50 of 5 and 4 nM, also potently inhibits ABL1 H396P (IC50=1.4 nM).
DCC-2036 inhibits cellular proliferation of Ba/F3 cells expressing native or T315I mutant with IC50 of 5.4 and 13 nM, also inhibits proliferation of several common TKI-resistant mutants of BCR-ABL1, including G250E, Q252H, Y235F, E255K, V299L, F317L, and M351T with IC50 of 6-150 nM.
DCC-2036 prolongs survival in mouse Ba/F3 cell allograft models.

物理化学性质&存储条件

分子量	553.5869
分子式	C30H28FN7O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Pyridinecarboxamide, 4-[4-[[[[3-(1,1-dimethylethyl)-1-(6-quinolinyl)-1H-pyrazol-5-yl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-

参考文献

1. Chan WW, et al. Cancer Cell. 2011 Apr 12;19(4):556-68.

2. Eide CA, et al. Cancer Res. 2011 May 1;71(9):3189-95.

3. O'Hare T, et al. Blood. 2011 Nov 10;118(19):5250-4.

4. O'Hare T, et al. Clin Cancer Res. 2011 Jan 15;17(2):212-21.

DCC-2036 (Rebastinib;DCC 2036;DCC2036)

生物&药学活性

物理化学性质&存储条件

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DCC-2036 (Rebastinib;DCC 2036;DCC2036)

生物&药学活性

物理化学性质&存储条件

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