Luvixasertib_product_DataBase

Bioactivity

CFI-402257 is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 has anti-cancer activity[1].

Target

IC50: 1.7 nM (TTK in vitro).

Invitro

CFI-402257 is highly selective to TTK. CFI-402257 is tested against a panel of human kinases at 1 μM and inhibits none of the 262 kinases tested. CFI-402257 is a potent inhibitor of cell growth[1]. CFI-402257 (200 nM, 6 h) causes a massive increase in chromosome missegregations[2].CFI-402257 (0, 50 or 100 nM) induces a dose-dependent dysregulation of the cell cycle, resulting in an increase in the frequency of cells exhibiting an aneuploid DNA content[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Luvixasertib 相关抗体: Cell Cycle Analysis[2] Cell Line:

In Vivo

CFI-402257 given orally QD shows dose-dependent activity in mice with established tumors from xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice. CFI-402257 demonstrates antitumor activity in a platinum-resistant PDX model of high-grade serous ovarian cancer[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

CAS

1610759-22-2

Formula

C28H30N6O3

Molar Mass

498.58

Appearance

固体

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671-5. [2]. Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132.

PeptideDB

Luvixasertib

CAS: 1610759-22-2 F: C28H30N6O3 W: 498.58