3- (5- fluoro- 4- (4- methyl- 2- (methylamino)thiazol- 5- yl)pyrimidin- 2- ylamino)benzenesulfonamide

10/01/2019 - "CDKI-73, one of the most potent and pharmacologically superior CDK9 inhibitors, has demonstrated excellent anti-tumour efficacy against several types of cancers. "
12/01/2022 - "Notably, in vivo evaluation showed that LS-007 significantly decreased the weight and volume of tumor and the expression of Ki67, promoted the expression of iNOS and inhibited the expression of CD206, suggesting that LS-007 might inhibit tumor growth by suppressing polarization of macrophages into tumor-associated macrophages (TAMs) in the TME. "
09/15/2014 - "As such, CDK9 inhibitor drug candidate CDKI-73 should have a major impact on these pathways in human cancers. "
01/01/2019 - "CDKI-73 induced cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. "
01/01/2019 - "In MV4-11 xenograft mouse models, oral administration of CDKI-73 resulted in a marked inhibition of tumor growth (p < 0.0001) and prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities. "

11/01/2016 - "In this study, we further evaluated the antitumor activity of LS-007 alone and in combination with a Bcl-2 inhibitor ABT-199 in acute leukemia (AL) cells. "
11/01/2016 - "Antitumor action of CDK inhibitor LS-007 as a single agent and in combination with ABT-199 against human acute leukemia cells."
01/30/2014 - "Furthermore, CDKI-73 was equipotent in poor prognostic sub-groups of leukemia patients and showed cytotoxic synergy with the nucleoside analog fludarabine. "
01/30/2014 - "CDKI-73 induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II. CDKI-73 was more potent than the pan-cdk inhibitor flavopiridol and showed >200-fold selectivity against primary leukemia cells when compared with normal CD34+ cells. "
01/30/2014 - "Cdk9 is a key elongation factor for RNA transcription and functions by phosphorylating the C-terminal domain of RNA polymerase II. Here we present direct evidence that cdk9 is important for cancer cell survival and describe the characterization of the potent cdk9 inhibitor CDKI-73 in primary human leukemia cells. "

04/01/2017 - "[Effect of CDK Inhibitor LS-007 on Acute Lymphoblastic Leukemia and Its Mechanism]."
04/01/2017 - "To study the effect of cyclin dependent kinase(CDK) inhibitor LS-007 on acute lymphoblastic leukemia and its mechanism. "
04/01/2017 - "LS-007 can affect the phosphorylation of RNA polymerase sites and promote cell apoptosis through changing the activities of CDK, thus having some positive significance for relieving acute lymphoblastic leukemia."
04/01/2017 - "quantitative PCR and Western blot detection showed that the levels of antiapoptotic protein decreased significantly in acute lymphoblastic leukemia cells after LS-007 treatment, and the pro-apoptotic effect of LS-007 combined with ABT-199 was much better. "
04/01/2017 - "The acute lymphocytic leukemia cell line was cultured and treated by LS-007, flavopiridol and ABT-199, then the changes of apoptosis-related factor mRNA and protein levels were detected by using mRNA quantitative PCR and Werstern blot. "

10/01/2019 - "Overall, this study provides compelling evidence that CDKI-73 is a promising drug candidate for treating colorectal cancer."

03/01/1988 - "[Clinical and microbiological study on effectiveness and usefulness of LS-007 for periodontitis]."