联系方式:
电话:021-58955995 手机:13611715263 联系人:客服部 Q Q:4008203792
ONC212产品描述:ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer drug and also a selective agonist of
GPR132.IC50 & Target: GPR132
[1]In Vitro: Cell proliferation assay reveals that at least a ten-fold lower concentration of ONC212 is needed to achieve 50% growth inhibition in comparison to ONC201. ONC212 shows GI
50 values in the range of 0.1 to 0.4 μM, while the corresponding ONC201 GI
50 values are in the range of 4 to 9 μM for the seven pancreatic cancer cell lines tested. Long-term cell proliferation assay shows that both ONC201 and ONC212 are comparable in inhibiting colony formation at a 20 ?M dose. However, at a 5 ?M dose, ONC212 is about 50-times more potent than ONC201 in preventing colony formation in four out of the seven pancreatic cancer cell lines tested. Induction of apoptosis by ONC212 is an earlier event than ONC201. Treatment with ONC201 and ONC212 reduces the expression of anti-apoptotic markers such as XIAP and MCL-1. Western blot analysis shows that in the HPAF-II cell line, ATF4 and phosphorylated EIF2α are upregulated as early as 6 to 12 hours post ONC201 or ONC212 treatment
[2].
In Vivo: Biweekly oral administration of 50 mg/kg ONC212 markedly inhibits Acute myeloid leukemia (AML) expansion and prolongs overall survival (p=0.0003). Median survival increases from 43 d in controls to 49 d in the ONC212-treated group (+14%)
[1]. ONC212 treatment exhibits significantly greater growth inhibition in comparison to ONC201. A dose of 50 mg/kg of ONC212 administered three-times a week is sufficient to lead to significant growth inhibition of tumors compare to the control group for these two models. Results demonstrate that ONC212 treated tumors show reduced proliferation in the HPAF-II model
[2].
In vivo toxicity assessment experiments show that ONC212 is well tolerated up to 250 mg/kg. 300 mg/kg of ONC212 causes splenic damage and elevates liver enzymes. ONC212 has a slightly shorter half-life than ONC201, with a clearance from the blood at 12 hours, T
1/2 of 4.3 hours, and C
max of 1.4 ?g/mL
[3].
产品链接:
www.medchemexpress.com/ONC212.html研究领域:
GPCR/G Protein 靶点:
GHSR相关产品:
Anamorelin |
Ibutamoren Mesylate |
Alexamorelin |
GHRP-2 metabolite 1 |
AZP-531 |
Capromorelin Tartrate |
Examorelin |
TC-G-1008 |
JMV 2959 |
TM-N1324 |
公司介绍:MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库,总部位于美国新泽西,分别在瑞典和上海设有欧洲区子公司和亚洲区总代理,营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商, 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域,PI3K、MAPK等近千个细分靶点,超过4000个活性小分子化合物现货,以及GPCR、API、离子通道等超过20种不同类型的化合物库,同时提供从毫克到千克的专业定制合成服务。MCE 对每批产品都进行严格的LCMS和NMR检验,其产品已被全球近万名客户广泛使用并发表大量文章、;MCE 定期增加各领域热门抑制剂、激动剂,不断扩增已有化合物库,以满足*新的科研需求;数千种产品在上海有充足备货,24-48小时内送达客户;大量产品提供免费试用装;已为全球多个知名企业、院校构建各种定制型化合物库。
联系方式:
电话:021-58955995 手机:13611715263 联系人:客服部 Q Q:4008203792