化合物Erismodegib diphosphate T15727

Product Introduction
Bioactivity


英文名: Sonidegib diphosphate

描述: Sonidegib diphosphate (LDE225 diphosphate) 是 Smo 的选择性拮抗剂，能够抑制鼠 Smo (IC50:1.3 nM)和人 Smo (IC50:2.5 nM)。

体外活性: Erismodegib diphosphate, a small molecule, clinically investigated SMO inhibitor. Erismodegib diphosphate is used alone and in combination with Nilotinib, inhibits the Hh pathway in CD34+ chronic phase (CP)-chronic myeloid leukaemia (CML) cells, reducing the number and self-renewal capacity of CML leukaemia stem cell (LSC). In a similar fashion to cyclopamine, Erismodegib interacts directly with SMO, to reduce the expression of downstream Hh signaling targets. The IC50 values for Erismodegib diphosphate for the major human CYP450 drug-metabolizing enzymes are greater than 10 μM. Primary CD34+ CP-CML cells are cultured in serum-free media (SFM)±Erismodegib for 6, 24, and 72 hours (h). At 72 h, while there is variability between the biological samples, GLI1 is obviously downregulated following exposure to Erismodegib (10 nM; 0.78-fold and 100 nM; 0.73-fold, respectively (p<0.01)[2].

体内活性: Erismodegib diphosphate is a weak base with a measured pKa of 4.2 and exhibits relatively poor aqueous solubility. Erismodegib diphosphate demonstrates dose-related antitumor activity after 10 days of oral administration of a suspension of the diphosphate salt, in the subcutaneous Ptch+/-p53-/- medulloblastoma allograft mouse model. Bone marrow cells and spleen cells from a subset of treated mice are transplanted into secondary recipient mice. Erismodegib diphosphate (5 mg/kg/day; once daily) obviously inhibits tumor growth, corresponding to a T/C value of 33% (p<0.05 as compared to vehicle controls). Erismodegib affords 51 and 83% regression respectively when dosed at 10 and 20 mg/kg/day qd [1]. Transplantation of either bone marrow (BM) or spleen cells from mice treated with Erismodegib diphosphate+ Nilotinib results in reduced white cell count (WCC) and reduces leukaemia development in secondary recipients compared to Erismodegib or Nilotinib alone[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 99 mg/mL(145.27 mM)
H2O : Insoluble


关键字: NVP-LDE225 diphosphate | LDE225 | LDE-225 | Erismodegib Diphosphate | Inhibitor | Smoothened | Sonidegib Diphosphate | Sonidegib diphosphate | Smo | Erismodegib | NVP-LDE-225 Diphosphate | inhibit | LDE 225 | LDE-225 Diphosphate | NVP-LDE 225 | NVP-LDE225 Diphosphate | Sonidegib | NVP-LDE-225 | NVP-LDE225 | LDE 225 Diphosphate | NVP-LDE 225 Diphosphate | LDE225 Diphosphate

相关产品: SAG | HhAntag | Taladegib | Halcinonide | JNJ-1289 | GI-560192 | IHR-1 | PF-5274857 | Jervine | MK-4101

相关库: Drug Repurposing Compound Library | Wnt/Hedgehog/Notch Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Clinical Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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