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Glasdegib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Glasdegib图片
CAS NO:1095173-27-5
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PF-04449913
产品介绍
Glasdegib 是一种口服具有活力的 Smoothened 抑制剂,能够结合到人Smo(181-787氨基酸位点),IC50=4 nM。

产品描述

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

体外活性

In vitro microsomal assays, PF-04449913 have high clearance in rat and low clearance in dog and human, without inhibiting any of the major cytochrome P450 isoforms. [1]

体内活性

In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability. [1]

细胞实验

PF-04449913 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Normal or BC CML CD34+ cells are plated on confluent mitomycin-C treated SL/M2 cells with vehicle, PF-04449913 (1 μM), Dasatinib (50 nM), or combination treatment. Mouse bone marrow stromal cell lines, M2-10B4 (M2) and SL/SL (SL) are treated with mitomycin-C (1 mg/mL) and plated in a 1:1 mixture at a total concentration of 100,000 cells/mL one day prior to co-culture with 10,000-20,000 CD34+ BC CML or normal progenitors. After 1 week of culture, progenitors are FACS sorted into hematopoietic progenitor assays and colonies are scored at 14 days. To assess survival of normal human hematopoietic stem and progenitor cells, irradiated (20 Gray) OP9 (M2 clone) stromal cells are co-cultured with 50,000 human CD34+ cord blood cells, vehicle or PF-04449913 in AlphaMEM with 20% Hyclone FBS, 1% pen strep glutamine and supplemented with 50 ng/mL SCF, 10 ng/mL thrombopoietin, and 10 ng/mL Flt3 and quantified by weekly FACS analysis[1].

Cas No.

1095173-27-5

分子式

C21H22N6O

分子量

374.448

别名

PF-04449913

储存和溶解度

DMSO:44 mg/mL (117.5 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years