ddr-in-1

DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family.

DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2.

DDR2-IN-1 (Compound 129) is recognized as a highly effective DDR2 inhibitor, displaying an IC50 value of 26 nM. It is a suitable choice for conducting osteoarthritis research.

S 16020-2 is an olivacine derivative, and DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors.

ATR-IN-23 (Compound 34), a potent and selective ATR inhibitor, exhibits an IC50 of 1.5 nM, has demonstrated antiproliferative effects on LoVo cells, and induces synthetic lethality in HT-29 cells, suggesting its utility in researching DNA damage response (DDR)-deficient cancers [1].

BTX161 is a Thalidomide analogue. BTX161 is a potent CKIα degrader. In human AML cells, BTX161 mediates the CKIα degradation better than Lenalidomide as well as activates DNA damage response (DDR) and p53, and also stabilizes the p53 antagonist MDM2[1].

DDR1-IN-6 is a potent and selective inhibitor of Discoidin Domain Receptor family member 1 (DDR1), exhibiting remarkable inhibitory activity at an IC50 of 9.72 nM. It effectively suppresses the auto-phosphorylation of DDR1b (Y513) with an IC50 value of 9.7 nM. Furthermore, DDR1-IN-6 displays strong anti-cancer activity.

DDR1-IN-5 is a potent and selective inhibitor of the Discoidin Domain Receptor family, member 1 (DDR1). It effectively inhibits the phosphorylation of DDR1b (Y513) with an IC 50 value of 4.1 nM. Furthermore, DDR1-IN-5 demonstrates remarkable anti-cancer activity. Its inhibitory potency against DDR1 (IC 50 = 7.36 nM) makes it a promising compound for targeted therapy in cancer treatment.

DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation. This compound demonstrates exceptional efficacy with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.

DDR1-IN-2 (DDR1 inhibitor 7rh) (DDR1 inhibitor 7rh) is a potent, selective, ATP-competitive Discoidin domain receptor 1 (DDR1) inhibitor (IC50: 6.8 nM in cell-free kinase assays).

Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide , with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].Phosphoramide mustard cyclohexanamine destroys rapidly dividing cells by forming NOR-G-OH, NOR-G and G-NOR-G adducts with DNA, potentially leading to DNA damage[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs)[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces DNA adduct formation[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces ovarian DNA damage in rat ovaries[1].Phosphoramide mustard cyclohexanamine increases DNA damage responses (DDR) gene (Atm, Parp1, Prkdc, Xrcc6, Brca1, Rad51) mRNA expression level[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) increased DDR proteins[1]. Cell Viability Assay[1] Cell Line: SIGCs Phosphoramide mustard cyclohexanamine (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats[2].Phosphoramide mustard cyclohexanamine (86.0 mg/kg; i.v.) has a plasma disappearance half-life of 15.1 minutes[2]. Animal Model: Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor[2] [1]. Shanthi Ganesan, et al. Phosphoramide mustard exposure induces DNA adduct formation and the DNA damage repair response in rat ovarian granulosa cells. Toxicol Appl Pharmacol. 2015 Feb 1; 282(3): 252-258. [2]. S Genka, et al. Brain and plasma pharmacokinetics and anticancer activities of cyclophosphamide and phosphoramide mustard in the rat. Cancer Chemother Pharmacol. 1990;27(1):1-7.