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Dasatinib Monohydrate
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。
Dasatinib Monohydrate图片
CAS NO:863127-77-9
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
BMS-354825 Monohydrate
产品介绍
Dasatinib (BMS-354825) monohydrate 是一种具有口服活性的，ATP 竞争性的，双重Src/Bcr-Abl抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的Ki值分别为 16 pM 和 30 pM。Dasatinib monohydrate 抑制Bcr-Abl和Src的IC50分别为<1.0 nM 和 0.5 nM。Dasatinib monohydrate 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。
生物活性

Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dualSrc/Bcr-Ablinhibitor with potent antitumor activity. TheKis are 16 pM and 30 pM forSrcandBcr-Abl, respectively. Dasatinib monohydrate inhibitsBcr-AblandSrcwithIC50s of<1.0 nM and 0.5 nM, respectively[1]. Dasatinib monohydrate also inducesapoptosisandautophagy.

IC50& Target[1]

Bcr-Abl

1.0 nM (IC50)

Src

0.5 nM (IC50)

lck

0.4 nM (IC50)

yes

0.5 nM (IC50)

c-kit

5.0 nM (IC50)

PDGFRβ

28 nM (IC50)

p38

100 nM (IC50)

Her1

180 nM (IC50)

Her2

710 nM (IC50)

FGFR-1

880 nM (IC50)

MEK

1700 nM (IC50)

体外研究
(In Vitro)

Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of<1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of<1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1].

体内研究
(In Vivo)

Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1].

Animal Model:Nude mice bearing K562 xenografts
Dosage:5 mg/kg and 50 mg/kg
Administration:Oral administration on a 5 day on and 2 day off schedule.
Result:Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model:Sprague-Dawley Rats
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral and i.v.
Result:Cmaxof 13.2 and 0.5 μM for i.v. and oral, respectively.
Clinical Trial
分子量

506.02

Formula

C22H28ClN7O3S

CAS 号

863127-77-9

中文名称

达沙替尼一水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.