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CAS No.: 939228-52-1

CCI-007 Catalog No. CSN27874

CCI-007 was identified as a compound that selectively and significantly decreased the viability of a subset of MLL-r and related leukemia cell lines with CALM-AF10 and SET-NUP214 translocation.

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生物活性

描述Mixed-lineage leukemia (MLL) gene rearrangements are among the most frequent chromosomal abnormalities in acute myeloid leukemia (AML)^[1].The most recurrent fusion partner in MLL rearrangements (MLL-r) is AF4, mapping at chromosome 4q21, accounting for approximately 36% of MLL-r leukemia and particularly prevalent in MLL-r acute lymphoblastic leukemia (ALL) cases (57%)^[2]. The systemic HRP-2 knockout mice only revealed an increase in neutrophils in the peripheral blood, whereas the depletion of Hepatoma-Derived Growth Factor-related protein 2(HRP-2) in leukemic cell lines and transformed primary murine cells resulted in reduced colony formation independently of MLL-rearrangements^[3].CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485. Small molecule CCI-007 was identified as a compound that selectively and significantly decreased the viability of a subset of MLL-r and related leukemia cell lines with CALM-AF10 and SET-NUP214 translocation. CCI-007 induced a rapid caspase-dependent apoptosis with mitochondrial depolarization within twenty-four hours of treatment. CCI-007 altered the characteristic MLL-r gene expression signature in sensitive cells with downregulation of the expression of HOXA9, MEIS1, CMYC and BCL2, important drivers in MLL-r leukemia, within a few hours of treatment. MLL-r leukemia cells that were resistant to the compound were characterised by significantly higher baseline gene expression levels of MEIS1 and BCL2 in comparison to CCI-007 sensitive MLL-r leukemia cells.^[4].
参考文献

[1] Hidemasa Matsuo,et al. Fusion partner-specific mutation profiles and KRAS mutations as adverse prognostic factors in MLL-rearranged AML. Blood Adv. 2020 Oct 13;4(19):4623-4631.
[2] Oliver Britten,et al. MLL-Rearranged Acute Leukemia with t(4;11)(q21;q23)-Current Treatment Options. Is There a Role for CAR-T Cell Therapy? Cells. 2019 Oct 29;8(11):1341.
[3] Siska Van Belle,et al. Unlike Its Paralog LEDGF/p75, HRP-2 Is Dispensable for MLL-R Leukemogenesis but Important for Leukemic Cell Survival. Cells. 2021 Jan 19;10(1):192.
[4] Somers K , Chudakova D A , Middlemiss S , et al. CCI-007, a novel small molecule with cytotoxic activity against infant leukemia with MLL rearrangements[J]. Oncotarget, 2016, 7(29):46067-46087.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9730 mL
- 14.8649 mL
- 29.7298 mL
- 5 mM
- 0.5946 mL
- 2.9730 mL
- 5.9460 mL
- 10 mM
- 0.2973 mL
- 1.4865 mL
- 2.9730 mL

技术信息

CAS号	939228-52-1	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C15H16N2O5S	运输	蓝冰
分子量	336.36	别名

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