AG-221(Enasidenib)

产品编号: DC8374 Featured
AG-221(Enasidenib)
结构式
1446502-11-9
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中国地区超过5000个高品质化合物库存
应用领域
Enasidenib是可口服,可逆,选择性的 IDH2 突变酶抑制剂,抑制IDH2R140Q 和 IDH2R172K 的 IC50 分别为100 和 400 nM。
Cas No.: 1446502-11-9
名称:
别名: AG221,AG 221
SMILES: C(NC1N=C(NCC(O)(C)C)N=C(C2C=CC=C(C(F)(F)F)N=2)N=1)1C=CN=C(C(F)(F)F)C=1
分子式: C19H17F6N7O
分子量: 473.14
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein, making it a highly targeted investigational medicine for the potential treatment of patients with cancers that harbor an IDH2 mutation. AG-221 has received orphan drug and fast track designations from the U.S. FDA. In September 2013, Agios initiated a Phase 1 multicenter, open-label, dose escalation clinical trial of AG-221 designed to assess the safety and tolerability of AG-221 in advanced hematologic malignancies. In October 2014, Agios initiated four expansion cohorts as part of the ongoing Phase 1 study and expanded its development program with the initiation of a Phase 1/2 study of AG-221 in advanced solid tumors. For the detailed information of AG-221, the solubility of AG-221 in water, the solubility of AG-221 in DMSO, the solubility of AG-221 in PBS buffer, the animal experiment (test) of AG-221, the cell expriment (test) of AG-221, the in vivo, in vitro and clinical trial test of AG-221, the EC50, IC50,and affinity,of AG-221, For the detailed information of AG-221, the solubility of AG-221 in water, the solubility of AG-221 in DMSO, the solubility of AG-221 in PBS buffer, the animal experiment (test) of AG-221, the cell expriment (test) of AG-221, the in vivo, in vitro and clinical trial test of AG-221, the EC50, IC50,and affinity,of AG-221, Please contact DC Chemicals.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC8374 AG-221(Enasidenib) Enasidenib是可口服,可逆,选择性的 IDH2 突变酶抑制剂,抑制IDH2R140Q 和 IDH2R172K 的 IC50 分别为100 和 400 nM。
DC8051 AG-120 (Ivosidenib) Ivosidenib (AG-120) 是异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 的口服活性抑制剂,它使 d-2- hydroxyglutatrate (2-HG) 在体内降低。Ivosidenib (AG-120) 具有良好的的安全性和临床活性,具有 AML 治疗的潜力。
DC12281 Olutasidenib (FT-2102) Olutasidenib (FT-2102) 是一种,具有口服活性的、能透过血脑屏障的、突变型异柠檬酸脱氢酶 (IDH)1 的选择性有效抑制剂,对IDH1- R132H 和 IDH1- R132C的 IC50 值分别为21.2 nM 和 114 nM。可用于治疗急性髓性白血病或骨髓增生异常综合征。
DC10439 Vorasidenib (AG881) Vorasidenib (AG-881) 是一种可口服的、脑渗透的第二代突变体异柠檬酸脱氢酶 1 和 2 (mIDH1/2) 双重抑制剂。Vorasidenib (AG-881) 以纳摩尔抑制 D-2-HG,对 IDH1 R132C、IDH1 R132G、IDH1 R132H、IDH1 R132S 的 IC50 值为 0.04~22 nM,对 IDH2 R140Q 值为 7~14 nM,对 IDH2 R172K 的值为 130 nM。