所有图片(2)
别名:
MPS1 Inhibitor, NMS-P715, (N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide)
经验公式（希尔记法）:
C35H39F3N8O3
推荐产品
product name
MPS1 Inhibitor, NMS-P715, The MPS1 Inhibitor, NMS-P715 controls the biological activity of MPS1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
质量水平
检测方案
≥98% (HPLC)
形式
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 10 mg/mL, clear, colorless
运输
ambient
储存温度
2-8°C
SMILES字符串
CN(N=C1C(NC2=C(CC)C=CC=C2CC)=O)C3=C1CCC4=C3N=C(NC5=CC=C(C(NC6CCN(C)CC6)=O)C=C5OC(F)(F)F)N=C4
一般描述
An orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (<10 M), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50 = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~ 1 M), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss. Also available as a 5 mM solution in DMSO (Cat. No. 506313).
An orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (<10 µM), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50 = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~ 1 µM), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett.21, 4507.
Colombo, R., et al. 2011. Cancer Res.70, 10255.
Colombo, R., et al. 2011. Cancer Res.70, 10255.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Shangming Tang et al.
Nature, 606(7916), 930-936 (2022-04-28)
Chromothripsis is a catastrophic mutational process that promotes tumorigenesis and causes congenital disease1-4. Chromothripsis originates from aberrations of nuclei called micronuclei or chromosome bridges5-8. These structures are associated with fragile nuclear envelopes that spontaneously rupture9,10, leading to DNA damage when
Akshay Narkar et al.
Cell reports, 34(12), 108892-108892 (2021-03-25)
Most solid tumors are aneuploid, and p53 has been implicated as the guardian of the euploid genome. Previous experiments using human cell lines showed that aneuploidy induction leads to p53 accumulation and p21-mediated G1 cell cycle arrest. We find that
Prasad Trivedi et al.
Nature, 618(7967), 1049-1056 (2023-06-15)
Chromothripsis, the shattering and imperfect reassembly of one (or a few) chromosome(s)1, is an ubiquitous2 mutational process generating localized and complex chromosomal rearrangements that drive genome evolution in cancer. Chromothripsis can be initiated by mis-segregation errors in mitosis3,4 or DNA
Holly Merta et al.
Developmental cell, 56(24), 3364-3379 (2021-12-02)
Failure to reorganize the endoplasmic reticulum (ER) in mitosis results in chromosome missegregation. Here, we show that accurate chromosome segregation in human cells requires cell cycle-regulated ER membrane production. Excess ER membranes increase the viscosity of the mitotic cytoplasm to
Meenu Maan et al.
Biochimica et biophysica acta. Molecular cell research, 1868(3), 118929-118929 (2020-12-15)
Error-free progression through mitosis is critical for proper cell division and accurate distribution of the genetic material. The anaphase-promoting complex/cyclosome (APC/C) ubiquitin ligase regulates the progression from metaphase to anaphase and its activation is controlled by the cofactors Cdc20 and
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