NVP-LDE225(Erismodegib)

产品编号: DC8493 Featured
NVP-LDE225(Erismodegib)
结构式
956697-53-3
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中国地区超过5000个高品质化合物库存
应用领域
Erismodegib (Sonidegib) 是有效,选择性的 Smo 拮抗剂, 抑制鼠和人Smo的 IC50 分别为 1.3 nM 和 2.5 nM。
Cas No.: 956697-53-3
名称: [1,1'-Biphenyl]-3-carboxamide,N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-,rel-
别名: NVP-LDE225,LDE225
SMILES: C(C1=CC=C(OC(F)(F)F)C=C1)1=CC=CC(C(NC2=CC=C(N3C[C@@H](C)O[C@@H](C)C3)N=C2)=O)=C1C
分子式: C26H26F3N3O3
分子量: 485.5
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: LDE225 inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively. LDE225 is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood−brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment. LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice. For the detailed information of NVP-LDE225, the solubility of NVP-LDE225 in water, the solubility of NVP-LDE225 in DMSO, the solubility of NVP-LDE225 in PBS buffer, the animal experiment (test) of NVP-LDE225, the cell expriment (test) of NVP-LDE225, the in vivo, in vitro and clinical trial test of NVP-LDE225, the EC50, IC50,and Affinity of NVP-LDE225, Please contact DC Chemicals.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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