7-Benzyl-4-(4-(trifluoromethyl)benzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one
ONC212
CAS: 1807861-48-8
Molecular Formula: C24H23F3N4O
7-Benzyl-4-(4-(trifluoromethyl)benzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one - Names and Identifiers
7-Benzyl-4-(4-(trifluoromethyl)benzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one - Physico-chemical Properties
| Molecular Formula | C24H23F3N4O |
| Molar Mass | 440.46 |
| Storage Condition | Room Temprature |
| In vitro study | ONC212 has Anti proliferative activity on many pancreatic cancer cell lines, more than 10 times higher than the efficacy of onc201. In sensitive pancreatic cancer cell lines, ONC212 induced apoptosis earlier than ONC201, and the effective concentration was lower. ONC212 has potent pro-apoptotic activity in acute myeloid leukemia and mantle cell lymphoma cell lines (ED50 141 nM in OCI-AML3 cells of p53 wild type, ED50 was 105.7 nM in MOLM13 cells and 265.2 nM in JeKo-1 cell lines). Time course analysis of apoptosis in OCI-AML3 cells found that ONC212 takes more than 36 hours to start inducing apoptosis. ONC212 can significantly induce Sub-G1 cell apoptosis or cause cell cycle arrest. |
| In vivo study | In melanoma and hepatocellular carcinoma xenograft models, ONC212 has significant efficacy. In colon cancer and triple-negative breast cancer, ONC212 has a broad therapeutic time window, an acceptable pharmacokinetic profile, oral tolerance in mice, and no apparent toxicity at effective doses. The activity of ONC212 has rapid kinetic characteristics. Its Half-Life is slightly shorter than that of ONC201, its clearance in blood is 12 hours, T 1/2 is 4.3 hours, and its Cmax is 1.4 mg/ml. Despite the effects of systemic clearance in vivo, the efficacy of ONC212 is relatively prolonged and oral ONC212 has potent antitumor activity in xenograft models of human melanoma and liver cancer. ONC206 and ONC201 could inhibit the invasion and migration of tumor cells, while ONC212 only inhibited the invasion. |
7-Benzyl-4-(4-(trifluoromethyl)benzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one - References
| biological activity | ONC212 is a fluorinated ONC201 analog that is a selective agonist of gpr132. ONC212 has broad efficacy in the low nanomolar range for most solid tumors and hematologic malignancies, and has potent anti-leukemic activity. |
| Target | GPR132 |
Last Update：2024-04-09 21:04:16
![7-Benzyl-4-(4-(trifluoromethyl)benzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one](http://res.chembk.com/assets/str/2d/1/18/1807861-48-8.png)
Supplier List
Product Name: ONC212 Visit Supplier Webpage Request for quotation
CAS: 1807861-48-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1807861-48-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: ONC212 Visit Supplier Webpage Request for quotation
CAS: 1807861-48-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1807861-48-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History