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c-Kit
转化生长因子-β Bcr-Abl 类器官培养添加剂
/ Dasatinib

达沙替尼 /Dasatinib {[allProObj[0].p_purity_real_show]}

货号：A355193 同义名： BMS-354825;Sprycel

Dasatinib是一种强效的双重 Abl/Src 抑制剂，IC50 分别为 < 1 nM 和 0.8 nM，并且还抑制 c-Kit（WT）/c-Kit（D816V）活性，IC50 分别为 79 nM 和 37 nM。

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Dasatinib 化学结构 CAS号：302962-49-8
Dasatinib 化学结构
CAS号：302962-49-8
Dasatinib 3D分子结构
CAS号：302962-49-8
Dasatinib 化学结构 CAS号：302962-49-8
Dasatinib 3D分子结构 CAS号：302962-49-8
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Dasatinib 纯度/质量文件 产品仅供科研

货号：A355193 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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更多 >
产品名称 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

 		99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		99% (HPLC)
Ki8751 ++

c-Kit, IC50: 40 nM

 		99%
Tivozanib ++

c-Kit, IC50: 78 nM

 		99%+
Pazopanib +

c-Kit, IC50: 140 nM

 		99%
Sitravatinib +++

Kit, IC50: 6 nM

 		99%+
Pexidartinib +++

Kit, IC50: 10 nM

 		99%+
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

 		99%
Axitinib ++++

Kit, IC50: 1.7 nM

 		98%
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 99%+
Sunitinib ✔ FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

 		99%+
Telatinib ++++

c-Kit, IC50: 1 nM

 		99%+
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
Dasatinib ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

 		Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

 		++++

ALK2, IC50: 1.3 nM

 		+

ALK3, IC50: 85.8 nM

 		+

ALK4, IC50: 2133 nM

 		+

ALK5, IC50: 9276 nM

 		99%+
ML347 ++

ALK1, IC50: 46 nM

 		++

ALK2, IC50: 32 nM

 		98%
K02288 ++++

ALK1, IC50: 1.8 nM

 		++++

ALK2, IC50: 1.1 nM

 		++

ALK3, IC50: 34.4 nM

 		+++

ALK6, IC50: 6.4 nM

 		99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%
LDN-214117 ++

ALK2, IC50: 24 nM

 		98%
DMH-1 +

ALK2, IC50: 107.9 nM

 		99%+
SB-505124 +

ALK4, IC50: 129 nM

 		++

ALK5, IC50: 47 nM

 		99%+
Vactosertib +++

ALK4, IC50: 13 nM

 		+++

ALK5, IC50: 11 nM

 		99%+
Alantolactone ✔ 98%
SIS3 ✔ 97%
Pirfenidone ✔ 98%
Hesperetin ✔ 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

 		98%
GW788388 +++

ALK5, IC50: 18 nM

 		98%
LY364947 ++

TGFβRI, IC50: 59 nM

 		+

TGFβRII, IC50: 0.4 μM

 		98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

 		99%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

 		99%+
LY2109761 ++

TβRI, Ki: 38 nM

 		+

TβRII, Ki: 300 nM

 		99%+
Galunisertib ++

TβRI, IC50: 56 nM

 		98%
SB 431542 +

ALK5, IC50: 94 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Abl ↓ Bcr-Abl ↓ 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

 		99%+
KW-2449 +++

Abl (T315I), IC50: 4 nM

Abl, IC50: 14 nM

 		FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

 		98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

 		c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

 		RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

 		FLT3,Tie-2 99%+
PP121 ++

Abl, IC50: 18 nM

 		VEGFR,PDGFR 99%+
GNF-7 +++

E255V, IC50: 122 nM

M351T, IC50: 133 nM

 		99%+
Olverembatinib dimesylate ++++

Abl (G250E), IC50: 0.35 nM

Abl, IC50: 0.34 nM

 		99%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

 		Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

 		Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

 		98+%
GNF-2 +

Bcr-Abl (K562 cell line), IC50: 273 nM

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

 		98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

 		DUB 98+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

 		99%
Radotinib ++

BCR-ABL1, IC50: 34 nM

 		98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dasatinib 生物活性

靶点

  • c-Kit

    c-Kit (D816V), IC50:37 nM

    c-Kit (wt), IC50:79 nM

  • Src

    Src, IC50:0.8 nM

  • Abl

    Abl, IC50:0.6 nM
描述 The oncogenic tyrosine kinase Bcr-Abl plays a central role in the pathogenesis of chronic myelogenous leukemia, thus makes it as the therapy drug target. However, it is demonstrated that the mutations of Bcr-Abl kinase have been the most common mechanism of drug resistance, such as imatinib. Dasatinib is a potent Bcr-Abl inhibitor with IC50 values of 0.6 nM, 0.8 nM and 2.8 nM for Abl, Src and Lyn, as well as IC50 values ranging in 0.1 - 1.8 nM for different Abl mutations except the T315l mutation (measured by in vitro kinase assays). Consistent with the results from the kinase assays, dasatinib showed more potent growth inhibition in Ba/F3 expressing various Abl mutations with a narrow range of low nanomoles, as well as the inhibition on Bcr-Abl tyrosine phosphorylation with IC50 values below 10 nM，compared with imatinib[1] Oral administration of Dasatinib at dose of 5 or 20 mg/kg robustly reduced the CML phenotype and included stem and progenitor populations in tetracycline-controlled transgenic BCR-ABL mice, more potent than imatinib[2]. Dasatinib also showed inhibitory activity against Lck, yes and c-kit with IC50 values of 0.4 nM, 0.5 nM and 5 nM, respectively, and possessed cellular antiproliferative activities on tumor cells of different origins, most potent to CML cell line K562 with IC50 < 1 nM. Oral treatment with Dasatinib, at dose of both 5 mg/kg and 50mg/kg on a 5 day on and 2 day off schedule for two cycles, demonstrated complete tumor regressions in a K562 xenograft model of CML[3].
作用机制 Dasatinib is a ATP-competitive inhibitor of both Abl and Src[4].

Dasatinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=0.19987 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.15458 μM SANGER
A101D Growth Inhibition Assay IC50=1.03043 μM SANGER
A253 Growth Inhibition Assay IC50=3.73246 μM SANGER

Dasatinib 动物研究

Dose Mice[5]: 1.5 mg/kg (i.v.), 1.25 mg/kg - 5 mg/kg (p.o.)
Administration i.v., p.o.
Pharmacokinetics
Animal Mice[6] Rats[6] Dogs[6] Monkeys[6]
Dose 5 mg/kg 10 mg/kg 3 mg/kg 5 mg/kg
Administration p.o. p.o. p.o. p.o.
Cmax 0.051 μg/ml 0.24 ± 0.09 μg/ml 0.14 ± 0.04 μg/ml 0.17 ± 0.03 μg/ml
T1/2 2.5 h 3.1 ± 0.3 h 5.0 ± 1.8 h 2.2 ± 0.4 h
AUC0→∞ 0.22 μg·h/ml 1.9 ± 1.0 μg·h/ml 0.68 ± 0.17 μg·h/ml 0.37 ± 0.02 μg·h/ml
F 0.17 27 ± 15 (%) 34 ± 13 (%) 15 ± 2 (%)
Tmax 2 h 2.3 ± 3.3 h 0.75 ± 0.25 h 0.6 ± 0.1 h

Dasatinib 参考文献

[1]O'Hare T, Walters DK, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005 Jun 1;65(11):4500-5.

[2]Dasatinib Exerts Differential Effects on Normal and BCR-ABL Positive Hematopoietic Cells in a Transgenic Mouse Model of Chronic Phase-CML

[3]Lombardo LJ, Lee FY, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61.

[4]Reddy EP, Aggarwal AK, et al. The ins and outs of bcr-abl inhibition. Genes Cancer. 2012 May;3(5-6):447-54.

[5]Luo FR, Yang Z, et al. Dasatinib (BMS-354825) pharmacokinetics and pharmacodynamic biomarkers in animal models predict optimal clinical exposure. Clin Cancer Res. 2006 Dec 1;12(23):7180-6.

[6] Pharmacokinetics of dasatinib

Dasatinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.25mL

2.05mL

1.02mL

20.49mL

4.10mL

2.05mL

Dasatinib 技术信息

CAS号302962-49-8
分子式C22H26ClN7O2S
分子量 488.005
别名 BMS-354825;Sprycel
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 120 mg/mL(245.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

4% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

Tags: Dasatinib | BMS-354825;Sprycel | Bcr-Abl | c-Kit | TGF-beta/Smad | AmBeed-信号通路专用抑制剂 | Dasatinib 纯度/质量文件 | Dasatinib 亚型比较 | Dasatinib 生物活性 | Dasatinib 细胞研究 | Dasatinib 动物研究 | Dasatinib 参考文献 | Dasatinib 实验方案 | Dasatinib 技术信息

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