Ethynylcytidine, DNA 定向 RNA 聚合酶 III 亚基 RPC1 抑制剂

小分子

乙炔胞苷

4-amino-1-[(2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one | TAS 106 [WHO-DD] | UNII-Y3O05I09ZK | AS-35187 | ethynylcytidine | 2(1H)-Pyrimidinone, 4-amino-1-(3-C-ethynyl-.beta.-D-ribofuranosyl)- | SB-596168; TAS-106; ECy

Ethynylcytidine

E651387-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis , inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer In Vitro The IC 50 values of Ethynylcytidine in the five human tumors with 4, 24 and 72 h exposure range from 0.114 to 1.032 μM, 0.015 to 0.067 μM, and 0.008 to 0.058 μM, respectively. These results suggest that the cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The differences in IC 50 values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appeares to show sufficiently potent cytotoxicity at the 24 h exposure time in all 5 human tumors. Even at the 4 h exposure time, Ethynylcytidine clearly shows potent cytotoxicity with IC 50 values at submicromolar concentrations in 4 of the 5 human tumors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with an tumor growth inhibition rate (IR) on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine (TAS-106) on all three administration schedules. In particular, administration of Ethynylcytidine at 6 mg/kg once weekly exhibits a marked tumor shrinking effect with an IR of 98% against the LX-1 tumor. While Ethynylcytidine treatment on an either 3 or 5 times weekly schedule has a potent antitumor effect with an IR of approximately 85%, the IR of Ethynylcytidine once weekly is less than 60% and its antitumor effect is rather weak . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:nucleoside antimetabolite

乙炔胞苷（ECyD）是一种核苷类似物，也是一种有效的 RNA 合成抑制剂，可抑制 RNA 聚合酶 I、II 和 II。乙炔胞苷在多种癌症模型中具有强大的抗肿瘤活性。

180300-43-0

C11H13N3O5

267.24 g/mol

176885

C#C[C@]1([C@H](O[C@H]([C@@H]1O)N2C=CC(=NC2=O)N)CO)O

4-amino-1-[(2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one

1S/C11H13N3O5/c1-2-11(18)6(5-15)19-9(8(11)16)14-4-3-7(12)13-10(14)17/h1,3-4,6,8-9,15-16,18H,5H2,(H2,12,13,17)/t6-,8+,9-,11-/m1/s1

JFIWEPHGRUDAJN-DYUFWOLASA-N

C#CC1(C(OC(C1O)N2C=CC(=NC2=O)N)CO)O

176885

DMSO : 250 mg/mL (935.49 mM; Need ultrasonic)

4

5

3

267.086 Da

267.086 Da

129.000 Ų

19

0

508.000

0

1

-2.700

-2.7

抑制剂

DNA 定向 RNA 聚合酶 III 亚基 RPC1 抑制剂