CC-671

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CC-671 是一种有效的、选择性的双重 TTK (Mps1)/CLK2 抑制剂，IC50 分别为 5/3 nM。

CC-671 is a potent, selective, dual TTK (Mps1)/CLK2 inhibitor with IC50 of 5/3 nM, respectively; weakly inhibits DYRK3, DYRK1A, PHKG, DYRK1B, and CLK1 with IC50 of 0.1-0.3 uM, and displays excellent kinase selectivity (7/235 kinases > 80% inhibition at 3 uM); inhibits autophosphorylation of TTK at T686 or phosphorylation of SR protein 75 with IC50 of 0.057 and 0.549 uM in Cal-51 cells; demonstrates strong single agent in vivo efficacy in multiple TNBC xenograft models without significant body weight loss.Breast Cancer Preclinical.

CC-671 (compound 23) is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively. HCT-116 cell lysates treated with CC-671 at 3 μM for 1 h demonstrates that only four kinases show cellular binding of 75% or more including CLK2, CAMKK2, PIP4K22, and JNK.

CC-671 (compound 23) demonstrates significant tumor growth inhibition (TGI) ((vehicle -treated/vehicle) ×100%) of 71% at both 10 and 20 mg/kg on a every 3 days (q3d) dosing schedule. The body weight loss (BWL) in the CC-671 treated group (20 mg/kg ) is higher than in the 10 mg/kg group (17% vs 5%).

CC671 | CC 671

Cell Cycle/DNA Damage

Mps1/TTK

CLK2|TTK

Cancer

Breast Cancer

1618658-88-0

512.57

C28H28N6O4

>98% (HPLC)

DMSO: 60 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(NC)C1=CC=C(NC2=NC(OC3CCCC3)=C4C(NC=C4C5=CC=C6N=C(C)OC6=C5)=N2)C(OC)=C1

4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7H-pyrrolo-[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-N-methylbenzamide

(-20℃)

With Ice Pack

≥ 2 years