Dasatinib (BMS-354825) - Moligand™, 10mM in DMSO , Bcr/Abl fusion protein, CAS No.302962-49-8, Bcr/Abl fusion protein

CAS: 302962-49-8 Cat. No.: D407815 Molecular Weight: 488.01 EC Number: 801-607-0
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GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Storage
Store at -80°C
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D407815-1ml
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 23 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

Information


In vitro

Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. Dasatinib has a two-log (∼325-fold) increased potency relative to imatinib. Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range. Dasatinib directly targets wild-type and mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl. The percent of colonies of TgE bone marrow cells are decreased from 100% in untreated wells to 4.12% in Dasatinib treated wells. In the presence of Dasatinib, the difference in the percentage of colonies formed by WT and TgE bone marrow cells is statistically significant. Expression of LMP2A is able to promote B lymphocyte survival and proliferation, which can be inhibited by targeting Lyn and/or c-Abl kinases through Dasatinib. Dasatinib treatment inhibits Src signaling, decreases growth, and induces cell cycle arrest and apoptosis in a subset of thyroid cancer cells. Treatment with increasing doses of Dasatinib (0.019 μM to 1.25 μM) for 3 days inhibits the growth of the C643, TPC1, BCPAP, and SW1736 cell lines by about 50% at low nanomolar concentrations, while higher concentrations are required to inhibit the growth of the K1 cell line. Treatment with 10 nM or 50 nM Dasatinib results in a 9-22% increase of cells in the G1 population among BCPAP and SW1736 and K1 cells, and a corresponding 7-18% decrease in the percentage of cells in the S phase.

In vivo

Dasatinib reverses splenomegaly in LMP2A/MYC double transgenic mice. Dasatinib specifically prevents colony formation by LMP2A expressing bone marrow B cells and decreased spleen size in the TgE mice. Spleen mass is significantly decreased among Dasatinib treated Tg6/λ-MYC mice when compared to the control group. Dasatinib inhibits lymphadenopathy in LMP2A/MYC double transgenic mice. Dasatinib reverses splenomegaly in Rag1KO mice engrafted with tumor cells from LMP2A/MYC double transgenic mice. Dasatinib therapy inhibits Lyn phosphorylation in B lymphocyte tumors expressing LMP2A.
Cell Data

cell lines:

Concentrations:~32 nM

Incubation Time:72 hours

Powder Purity:≥99%

Specifications

Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Bcr/Abl fusion protein
Product Properties
ALogP3.6
Names and Identifiers
Isomeric SMILES CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO
Alternate CAS 302962-49-8,863127-77-9
NSC Number 732517
MeSH Entry Terms (18F)-N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide;354825, BMS;BMS 354825;BMS-354825;BMS354825;dasatinib;N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methyl
Molecular Weight 488.01
Reaxy-Rn 9966762
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9966762&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

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✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

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📊 Datasheet

Quick-reference summary of product specifications and applications.

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🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

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Advanced Data

Associated Targets(Human)
CSK Tchem Tyrosine-protein kinase CSK (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA2 Tclin Ephrin type-A receptor 2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA4 Tchem Ephrin type-A receptor 4 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA8 Tchem Ephrin type-A receptor 8 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHB1 Tchem Ephrin type-B receptor 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHB4 Tchem Ephrin type-B receptor 4 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA5 Tchem Ephrin type-A receptor 5 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHB6 Tchem Ephrin type-B receptor 6 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ERBB3 Tclin Receptor tyrosine-protein kinase erbB-3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DDR2 Tchem Discoidin domain-containing receptor 2 (9 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA1 Tchem Ephrin type-A receptor 1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGFR Tclin Epidermal growth factor receptor (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA3 Tchem Ephrin type-A receptor 3 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DDR1 Tchem Epithelial discoidin domain-containing receptor 1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PTK6 Tchem Protein-tyrosine kinase 6 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SRMS Tchem Tyrosine-protein kinase Srms (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SRC Tclin Proto-oncogene tyrosine-protein kinase Src (20 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TXK Tchem Tyrosine-protein kinase TXK (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
YES1 Tclin Tyrosine-protein kinase Yes (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FRK Tchem Tyrosine-protein kinase FRK (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FYN Tclin Tyrosine-protein kinase Fyn (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHB2 Tchem Ephrin type-B receptor 2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GAK Tchem Cyclin-G-associated kinase (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGR Tchem Tyrosine-protein kinase Fgr (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIK1 Tchem Serine/threonine-protein kinase SIK1 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIK2 Tchem Serine/threonine-protein kinase SIK2 (7 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TEC Tchem Tyrosine-protein kinase Tec (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIK3 Tchem Serine/threonine-protein kinase SIK3 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PKMYT1 Tchem Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRA Tclin Platelet-derived growth factor receptor alpha (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRB Tclin Platelet-derived growth factor receptor beta (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LCK Tclin Tyrosine-protein kinase Lck (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LYN Tclin Tyrosine-protein kinase Lyn (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BTK Tclin Tyrosine-protein kinase BTK (7 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BMX Tchem Cytoplasmic tyrosine-protein kinase BMX (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BCR Tclin Breakpoint cluster region protein (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BLK Tchem Tyrosine-protein kinase Blk (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNK2 Tclin Activated CDC42 kinase 1 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL2 Tchem Tyrosine-protein kinase ABL2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL1 (37 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNNI3K Tchem Serine/threonine-protein kinase TNNI3K (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HCK Tclin Tyrosine-protein kinase HCK (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KIT Tclin Mast/stem cell growth factor receptor Kit (22 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAPK14 Tchem Mitogen-activated protein kinase 14 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MYT1 Tchem Myelin transcription factor 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificates(CoA,COO,BSE/TSE and Analysis Chart)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemical and Physical Properties
SolubilitySolubility (25°C) In vitro DMSO: 46 mg/mL (196.35 mM); Ethanol: 13 mg/mL warmed with 50ºC Water: bath (55.49 mM); Water: Insoluble;
Melt Point(°C)280 °C
Documents & Articles
Citations of This Product
References
1. Xiaofei Zhang, Mengyuan Lv, Yuyang Wang, Nan Zhang, Di Chen.  (2025)  Inner-wall biochar-coated pipette tip microextraction for rapid and sustainable determination of tyrosine kinase inhibitors in plasma.  RSC Advances,  15  (40): (33536-33548).  [PMID:40959299] [10.1039/D5RA05405B]
2. Zhiming Wang, Jing Tan, Mengxuan Li, Can Gao, Wenwen Li, Jing Xu, Changchuan Guo, Zhenzhen Chen, Rong Cai.  (2023)  Clickable Photoreactive ATP-Affinity Probe for Global Profiling of ATP-Binding Proteins.  ANALYTICAL CHEMISTRY,      [PMID:37993803] [10.1021/acs.analchem.3c02694]
3. Yao Liu, Zhichao He, Heng Liang, Minzhen Han, Jinxingyi Wang, Qian Liu, Yanping Guan.  (2023)  A high-throughput UHPLC-MS/MS method for the determination of eight anti-tumor drugs in plasma.  ANALYTICAL BIOCHEMISTRY,      [PMID:37429484] [10.1016/j.ab.2023.115230]
4. Lu Yang, Jiaxi Xu, Zheng Xie, Faquan Song, Xin Wang, Rupei Tang.  (2021)  Carrier-free prodrug nanoparticles based on dasatinib and cisplatin for efficient antitumor in vivo.  Asian Journal of Pharmaceutical Sciences,      [PMID:35027952] [10.1016/j.ajps.2021.08.001]
5. Zhao-Yang Wang, Hai-Long Wu, Yue-Yue Chang, Tong Wang, Wei Chen, Gao-Yan Tong, Ru-Qin Yu.  (2021)  Simultaneous determination of nine tyrosine kinase inhibitors in three complex biological matrices by using high-performance liquid chromatography–diode array detection combined with a second-order calibration method.  JOURNAL OF SEPARATION SCIENCE,  44  (21): (3914-3923).  [PMID:34463059] [10.1002/jssc.202100293]
6. Deng-Pan Wu, Yan Zhou, Li-Xiang Hou, Xiao-Xiao Zhu, Wen Yi, Si-Man Yang, Tian-Yu Lin, Jin-Lan Huang, Bei Zhang, Xiao-Xing Yin.  (2021)  Cx43 deficiency confers EMT-mediated tamoxifen resistance to breast cancer via c-Src/PI3K/Akt pathway.  International Journal of Biological Sciences,      [PMID:34326682] [10.7150/ijbs.55453]
7. Dawei Yang, Xiaoyu Tian, Yuchen Ye, Yin Liang, Jie Zhao, Tao Wu, Na Lu.  (2021)  Identification of GL-V9 as a novel senolytic agent against senescent breast cancer cells.  LIFE SCIENCES,      [PMID:33617857] [10.1016/j.lfs.2021.119196]
8. Qingqing Li, Xianwei Yang, Peipei Zhang, Fei Mo, Peiru Si, Ximeng Kang, Menghan Wang, Jiye Zhang.  (2021)  Dasatinib loaded nanostructured lipid carriers for effective treatment of corneal neovascularization.  Biomaterials Science,  (7): (2571-2583).  [PMID:33589891] [10.1039/D0BM01599G]
9. Yue-Yue Chang, Hai-Long Wu, Huan Fang, Tong Wang, Yang-Zi Ouyang, Xiao-Dong Sun, Gao-Yan Tong, Yu-Jie Ding, Ru-Qin Yu.  (2020)  Comparison of three chemometric methods for processing HPLC-DAD data with time shifts: Simultaneous determination of ten molecular targeted anti-tumor drugs in different biological samples.  TALANTA,      [PMID:33379025] [10.1016/j.talanta.2020.121798]
10. Qianqian Wang, Yuanyuan Zheng, Bowen Deng, Di Chen, Liuqun Jia, Nian Shi.  (2024)  Automated kapok fiber-based pipette-tip solid-phase extraction coupled with liquid chromatography-tandem mass spectrometry for rapid and sensitive analysis of tyrosine kinase inhibitors in plasma.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:39378625] [10.1016/j.chroma.2024.465420]
11. Lisha Liu, Beiyuan Zhang, Xianggui Wu, Gang Cheng, Xiaopeng Han, Xiaofei Xin, Chao Qin, Lei Yang, Meirong Huo, Lifang Yin.  (2024)  Bioresponsive nanocomplex integrating cancer-associated fibroblast deactivation and immunogenic chemotherapy for rebuilding immune-excluded tumors.  Nanomedicine-Nanotechnology Biology and Medicine,      [PMID:38484918] [10.1016/j.nano.2024.102743]
12. Xiaolan Zhou, Xiaofeng Zhu, Weixu Wang, Jing Wang, Haimei Wen, Yuqi Zhao, Jiayu Zhang, Qiushi Xu, Zhaozhao Zhao, Ting Ni.  (2025)  Comprehensive Cellular Senescence Evaluation to Aid Targeted Therapies.  Research,      [PMID:39822281] [10.34133/research.0576]
13. Jiaxing Lei, Lei Wang, Chen Yang, Dongdong Li, Jiaxue Zhang, Jia Ma, Peipei Zhang, Qingqing Li, Jiye Zhang.  (2024)  Dasatinib and erianin co-loaded ion-responsive in-situ hydrogel for effective treatment of corneal neovascularization.  JOURNAL OF CONTROLLED RELEASE,      [PMID:39368709] [10.1016/j.jconrel.2024.10.001]
14. Jing Ye, Yuanyuan Zheng, Xiangyu Li, Xingyi Jiang, Di Chen.  (2024)  Melt-blown polypropylene nonwoven as an efficient and eco-economic sorbent for pipette tip micro-solid phase extraction for the determination of tyrosine kinase inhibitors.  ANALYTICA CHIMICA ACTA,      [PMID:39396303] [10.1016/j.aca.2024.343240]
15. Qianqian Wang, Yuwei Liu, Yuanyuan Zheng, Di Chen, Ya Xie, Nian Shi.  (2024)  MonoTip C18 pipette tip solid-phase extraction coupled with liquid chromatography-tandem mass spectrometry enables rapid and automated therapeutic drug monitoring of tyrosine kinase inhibitors.  Arabian Journal of Chemistry,      [PMID:] [10.1016/j.arabjc.2024.105976]
16. Ninghong Li, Lu Liu, Dong Liu, Hengyi Yu, Guangjie Yang, Lihui Qiu, Yufei Chen, Dong Xiang, Xuepeng Gong.  (2024)  Simultaneous determination of three tyrosine kinase inhibitors and three triazoles in human plasma by LC-MS/MS: applications to therapeutic drug monitoring and drug-drug interaction studies.  JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,      [PMID:39208604] [10.1016/j.jchromb.2024.124276]
17. Haolin Song, Hongyi Chen, Qinjun Chen, Hongrui Fan, Chufeng Li, Yu Wang, Shilin Zhang, Xuwen Li, Boyu Su, Tao Sun, Chen Jiang.  (2024)  Size and Charge Dual-Switchable Nanoparticles for Achieving Chemosensitization and Immune Infiltration against Pancreatic Ductal Adenocarcinoma.  ADVANCED FUNCTIONAL MATERIALS,      [PMID:] [10.1002/adfm.202411643]
18. Dong Wang, Mengrong Li, Tingting Dai, Xiangyu Zhang, Di Chen.  (2025)  Sensitive analysis of tyrosine kinase inhibitors in plasma using polypropylene fabric-solid phase extraction combined with liquid chromatography-tandem mass spectrometry.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:40865307] [10.1016/j.chroma.2025.466315]
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21. Wang Dong, Li Mengrong, Zhang Xiangyu, Chai Shiwei, Chen Di.  (2026)  Ultrasonic-assisted magnetic sorbent–wrapped stick dip extraction enables batch-scale and green LC-MS/MS analysis of tyrosine kinase inhibitors in plasma.  ANALYTICAL AND BIOANALYTICAL CHEMISTRY,      [PMID:41575510] [10.1007/s00216-026-06335-2]
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