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Dasatinib/达沙替尼 {[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/达沙替尼 化学结构 CAS号：302962-49-8
Dasatinib/达沙替尼 化学结构
CAS号：302962-49-8
Dasatinib/达沙替尼 3D分子结构
CAS号：302962-49-8
Dasatinib/达沙替尼 化学结构 CAS号：302962-49-8
Dasatinib/达沙替尼 3D分子结构 CAS号：302962-49-8
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Dasatinib/达沙替尼 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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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

 		97%
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 (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 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 2HCl ++++

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%
(E/Z)-SIS3 free base ✔ 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, IC50: 14 nM

Abl (T315I), IC50: 4 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 +++

M351T, IC50: 133 nM

E255V, IC50: 122 nM

 		99%+
Olverembatinib dimesylate ++++

Abl, IC50: 0.34 nM

Abl (G250E), IC50: 0.35 nM

 		98%
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 (SUP-B15 cell line), IC50: 268 nM

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

 		98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

 		DUB/Deubiquitinase 99+%
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/达沙替尼 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/达沙替尼 细胞实验

Cell Line
Concentration Treated Time Description References
REH GCR cells 100 nM 48 h Dasatinib was the only inhibitor able to reduce the number of cells in this population when combined with dexamethasone, indicating its effectiveness in inhibiting active signaling in GC-resistant cells. Nat Commun. 2023 May 22;14(1):2935.
NALM6 cells 100 nM 48 h The combination of dexamethasone and dasatinib resulted in more apoptosis compared to treatment with dexamethasone or dasatinib alone in a dose-dependent manner, indicating its effectiveness in targeting active signaling in GC-resistant cells. Nat Commun. 2023 May 22;14(1):2935.
A375 cells 100 nM 24 h To assess the inhibitory effect of dasatinib on TCB-mediated target-cell killing, results showed that 100 nM dasatinib significantly inhibited target-cell killing J Immunother Cancer. 2021 Jul;9(7):e002582.
SKM-1 cells 100 nM 24 h To assess the inhibitory effect of dasatinib on TCB-mediated target-cell killing, results showed that 100 nM dasatinib significantly inhibited target-cell killing J Immunother Cancer. 2021 Jul;9(7):e002582.
PS125 3, 10 nM 1–24 h Dasatinib significantly reduced cell viability and induced G2/M phase cell cycle arrest. Cancer Lett. 2014 Nov 1;354(1):68-76.
D556 1, 5, 10, 50, 100 nM 1–24 h Dasatinib significantly reduced cell viability and induced G2/M phase cell cycle arrest. Cancer Lett. 2014 Nov 1;354(1):68-76.
DAOY 1, 5, 10, 50, 100 nM 1–24 h Dasatinib significantly reduced cell viability and induced G2/M phase cell cycle arrest. Cancer Lett. 2014 Nov 1;354(1):68-76.
A375 cells 100 nM 24 h To assess the inhibitory effect of dasatinib on TCB-mediated target-cell killing, results showed that 100 nM Dasatinib significantly inhibited target-cell killing. J Immunother Cancer. 2021 Jul;9(7):e002582.
SKM-1 cells 100 nM 24 h To assess the inhibitory effect of dasatinib on TCB-mediated target-cell killing, results showed that 100 nM Dasatinib significantly inhibited target-cell killing. J Immunother Cancer. 2021 Jul;9(7):e002582.
Human bone marrow mesenchymal stem cells (BM-MSCs) 1 μM 21 days Dasatinib inhibited the viability and adipogenesis commitment of human BM-MSCs, reducing adipocyte formation. Cardiovasc Diabetol. 2023 Aug 17;22(1):214.

Dasatinib/达沙替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice PC3/CD63-Antares2 xenograft model Intraperitoneal injection 5 mg/kg Once every 3 days for 35 days Evaluated dasatinib's inhibitory effect on tumor-derived exosome secretion, found low-dose dasatinib significantly reduced luminescence signals in blood and exosome-homing organs Sci Rep. 2020 Oct 6;10(1):16616
Mice NALM6-Luc+ xenograft model Oral 35 mg/kg Twice daily for 14 days Combination treatment resulted in a significant reduction of engraftment compared to vehicle, dexamethasone or dasatinib alone and increased survival, indicating its ability to overcome GC resistance. Nat Commun. 2023 May 22;14(1):2935.
NSG mice Humanized NSG mice Oral 50 mg/kg Twice daily for 2 days To assess the inhibitory effect of dasatinib on CD19-TCB-mediated B cell depletion and cytokine release, results showed that dasatinib significantly inhibited B cell depletion and cytokine release J Immunother Cancer. 2021 Jul;9(7):e002582.
Mice PS125 mouse MB model Oral 15 mg/kg Daily for 4 weeks Dasatinib treatment significantly reduced tumor volume with no observed toxicity. Cancer Lett. 2014 Nov 1;354(1):68-76.
NSG mice Humanized NSG mice Oral 50 mg/kg Twice daily for 2 days To evaluate the inhibitory effect of Dasatinib on CD19-TCB-mediated B cell depletion and cytokine release in vivo, results showed that Dasatinib significantly inhibited B cell depletion and cytokine release. J Immunother Cancer. 2021 Jul;9(7):e002582.
Mice Dbb mice (obese, type 2 diabetic model) Oral gavage 5 mg/kg Once per week for four weeks Dasatinib reduced lipid accumulation in the heart and bone marrow of diabetic mice, improved diastolic function, and reduced cardiac fibrosis. Cardiovasc Diabetol. 2023 Aug 17;22(1):214.

Dasatinib/达沙替尼 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/达沙替尼 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/达沙替尼 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/达沙替尼 技术信息

CAS号302962-49-8
分子式C22H26ClN7O2S
分子量 488.01
SMILES Code O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=C(C)C=CC=C4Cl
MDL No. MFCD11046566
别名 BMS-354825; Sprycel
运输蓝冰
InChI Key ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Pubchem ID 3062316
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
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四
方案 五
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一
方案 二
方案 三

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

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