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Dasatinib

Catalog No. T1448 CAS 302962-49-8

Synonyms: BMS-354825

Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.

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Dasatinib, CAS 302962-49-8

Pack Size	Availability	Price/USD
50 mg	In stock	$ 37.00
100 mg	In stock	$ 53.00
200 mg	In stock	$ 63.00
500 mg	In stock	$ 96.00
1 g	In stock	$ 139.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.89%

Purity: 99.86%

Purity: 99.62%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.
Targets&IC50	c-Kit (D816V):37 nM (cell free), Abl:0.6 nM (cell free), c-Kit (WT):79 nM (cell free), Src:0.8 nM (cell free)
In vitro	METHODS: Eight thyroid cancer cells were treated with Dasatinib (0.019-1.25 μmol/L) for 3 days, and cell proliferation was detected by SRB. RESULTS: The IC50 of Dasatinib on C643, TPC1, BCPAP, SW1736, K1, 8505C, HTh74 and HTh7 cells were 0.09, 0.03, 0.04, 0.08, 0.4, 2.7, >5 and 1.6 μmol/L, respectively.[1] METHODS: Human lung cancer cells NCI-H1975 and NCI-H1650 were treated with Dasatinib (2.5-20 μM) for 48 h. Apoptosis was detected by Flow Cytometry. RESULTS: Dasatinib induced apoptosis in NCI-H1975 and NCI-H1650 cells at 10 and 20 μM. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Dasatinib (50 mg/kg in 80 mmol/L sodium citrate buffer, pH 3.0) was administered orally to athymic nude mice harboring human thyroid carcinoma tumors of BCPAP or 8505C, five days per week for 20 days. RESULTS: Dasatinib significantly inhibited BCPAP tumors in situ, with final tumor volume suppressed by more than 90%. Dasatinib treatment did not significantly inhibit the growth of 8505C-derived tumors at any time point. [1] METHODS: To investigate the effects on neuroinflammation, Dasatinib (20 mg/kg in 4%DMSO+30%PEG+5%Tween 80) was administered intraperitoneally or orally to C57BL6/N mice once daily for four days, followed by intraperitoneal injection of LPS (10 mg/kg) to induce neuroinflammatory responses in vivo. RESULTS: Intraperitoneal injection and oral administration of Dasatinib inhibited LPS-induced activation of microglia/astrocytes, pro-inflammatory cytokine levels, and neutrophil rolling in the brains of wild-type mice. [3]
Kinase Assay	Kinase assays using wild-type and mutant glutathione S-transferase (GST)–Abl fusion proteins (c-Abl amino acids 220-498) were done as described, with minor alterations. GST-Abl fusion proteins were released from glutathione-Sepharose beads before use; the concentration of ATP was 5 μmol/L. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins were treated with LAR tyrosine phosphatase according to the manufacturer's instructions. After 1-hour incubation at 30°C, LAR phosphatase was inactivated by addition of sodium vanadate (1 mmol/L). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase was routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The inhibitor concentration ranges for IC50 determinations were 0 to 5,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The BMS-354825 concentration range was extended to 1,000 nmol/L for mutant T315I. These same inhibitor concentrations were used for the in vitro peptide substrate phosphorylation assays. The three inhibitors were tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase [1].
Cell Research	Ba/F3 cell lines were plated in triplicate and incubated with escalating concentrations of imatinib, AMN107, or BMS-354825 for 72 hours. Proliferation was measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90 determinations were 0 to 2,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The imatinib concentration range was extended to 6,400 nmol/L for mutants with IC50 >2,000 nmol/L. The BMS-354825 concentration range was extended to 200 nmol/L for mutant T315I [1].
Animal Research	For in vivo studies, dasatinib (50 mg/kg) was prepared for daily oral gavage (5 d/wk) in 80 mmol/L sodium citrate buffer, pH 3.0. For the orthotopic murine model, mice were randomized on day 10 based on bioluminescence activity to receive drug or vehicle. In the metastatic murine model, mice received dasatinib or vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following randomization (posttreatment) [4].

Synonyms	BMS-354825
Molecular Weight	488.01
Formula	C22H26ClN7O2S
CAS No.	302962-49-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 91 mg/mL (186.5 mM)

References and Literature

1. Chan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91. 2. Zhang M, et al. Dasatinib Inhibits Lung Cancer Cell Growth and Patient Derived Tumor Growth in Mice by Targeting LIMK1. Front Cell Dev Biol. 2020 Dec 4;8:556532. 3. Ryu KY, et al. Dasatinib regulates LPS-induced microglial and astrocytic neuroinflammatory responses by inhibiting AKT/STAT3 signaling. J Neuroinflammation. 2019 Oct 26;16(1):190. 4. Chan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91. 5. Shen Z, et al. Metabolite profiling of dasatinib dosed to Wistar Han rats using automated dried blood spot collection. J Pharm Biomed Anal. 2012 Aug-Sep;67-68:92-7. 6. Kan He, et al. Protein kinase inhibitors. Patent. US20180099960A1.

Citations

1. Cai Z, Wu X, Song Z, et al.Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis.Cell Discovery.2023, 9(1): 104. 2. Yan H, Wu W, Hu Y, et al.Regorafenib inhibits EphA2 phosphorylation and leads to liver damage via the ERK/MDM2/p53 axis.Nature Communications.2023, 14(1): 2756. 3. Liu K, Hao Z, Zheng H, et al.Repurposing of rilpivirine for preventing platelet β3 integrin-dependent thrombosis by targeting c-Src active autophosphorylation.Thrombosis Research.2023 4. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866. 5. Wang T, Yang C, Li Z, et al.Flavonoid 4, 4′-dimethoxychalcone selectively eliminates senescent cells via activating ferritinophagy.Redox Biology.2023: 103017. 6. Li F, Wang Z, Zheng D, et al.NK92 cells and peripheral blood NK cells respond oppositely upon dasatinib treatment.Immunology.2024

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library EMA Approved Drug Library Kinase Inhibitor Library Inhibitor Library FDA-Approved Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library

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Keywords

Dasatinib 302962-49-8 Angiogenesis Apoptosis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors c-Kit Bcr-Abl Src active antiproliferative CML antitumor breast Inhibitor prostate BMS354825 colon K562 BMS-354825 WiDr PC3 orally BMS 354825 inhibit inhibitor

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