| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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Purity: ≥98%
Dasatinib (formerly known as BMS-354825; sold under the brand name Sprycel), is a novel, potent and multi-targeted, orally bioavailable synthetic small molecule inhibitor that targets Abl, Src and c-Kit, with IC50 of<1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Chemotherapy patients treated with dasatinib may have acute lymphoblastic leukemia (ALL) or chronic myelogenous leukemia (CML). It is especially used to treat cases where the chromosome is positive for the Philadelphia gene (Ph+). The growth-promoting properties of these kinases are bound by dasatinib and inhibited. Dasatinib is able to reverse the resistance of chronic myeloid leukemia (CML) cells with point mutations in the BCR-ABL kinase domain to imatinib, presumably due to its less strict binding affinity for the BCR-ABL kinase.
| Targets |
Bcr-Abl (IC50 = 1 nM); Src (IC50 = 0.5 nM); lck (IC50 = 0.4 nM); Yes (IC50 = 0.5 nM); c-kit (IC50 = 5 nM); PDGFRβ (IC50 = 28 nM); p38 (IC50 = 100 nM); Her1 (IC50 = 180 nM); Her2 (IC50 = 710 nM); FGFR-1 (IC50 = 880 nM); MEK (IC50 = 1700 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Kinase assays are conducted with both wild-type and mutant glutathione S-transferase (GST)-Abl fusion proteins (c-Abl amino acids 220-498). Before usage, the GST-Abl fusion proteins are liberated from glutathione-Sepharose beads; 5 μM of ATP is present. The GST-Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase right before being used in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays. Sodium vanadate (1 mM) is added to inactivate LAR phosphatase following a 1-hour incubation period at 30°C. 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, immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase is routinely performed. The range of dasatinib concentrations for mutant T315I is increased to 1,000 nM. The in vitro peptide substrate phosphorylation assays employ the same concentrations of inhibitor. The three inhibitors are examined against GST-Src kinase and GST-Lyn kinase within these same concentration ranges.
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| Cell Assay |
Triple-seeded Ba/F3 cell lines are cultured for 72 hours at increasing dasatinib concentrations. A viability assay based on methanethiosulfonate is used to quantify proliferation. IC50 and IC90 values are given as the average of three separate, quadruple-experimented runs. The ranges of inhibitor concentrations (Dasatinib) are 0 nM to 32 nM. For mutant T315I, the dasatinib concentration range is expanded to 200 nM.
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| Animal Protocol |
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| References |
| Molecular Formula |
C22H26CLN7O2S.HCL
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| Molecular Weight |
524.47
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| Exact Mass |
523.1323997
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| CAS # |
854001-07-3
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| Related CAS # |
Dasatinib;302962-49-8;Dasatinib monohydrate;863127-77-9;Dasatinib-d8;1132093-70-9
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| Appearance |
Solid
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| SMILES |
CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.Cl
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| InChi Key |
MSCGWICDJYLQOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26ClN7O2S.ClH/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31;/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27);1H
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| Chemical Name |
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrochloride
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| Synonyms |
BMS-354825 HCl; BMS354825; BMS354825. Dasatinib HCl; Trade name: Sprycel
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.33 mg/mL (6.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 33.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.33 mg/mL (6.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 33.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3.33 mg/mL (6.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9067 mL | 9.5334 mL | 19.0669 mL | |
| 5 mM | 0.3813 mL | 1.9067 mL | 3.8134 mL | |
| 10 mM | 0.1907 mL | 0.9533 mL | 1.9067 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01660971 | Active Recruiting |
Drug: Dasatinib Drug: Erlotinib Hydrochloride |
Stage III Pancreatic Cancer AJCC v6 and v7 Recurrent Pancreatic Carcinoma |
National Cancer Institute (NCI) |
July 30, 2012 | Phase 1 |
| NCT01746836 | Recruiting | Drug: Ponatinib Hydrochloride Other: Quality-of-Life Assessment |
Philadelphia Chromosome Positive, BCR-ABL1 Positive Chronic Myelogenous Leukemia Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive |
M.D. Anderson Cancer Center | January 17, 2013 | Phase 2 |
| NCT03654768 | Active Recruiting |
Drug: Dasatinib Drug: Bosutinib |
Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive |
SWOG Cancer Research Network | October 24, 2018 | Phase 2 |
| NCT01398046 | Completed | Drug: Dasatinib plus Rabeprazole Drug: Dasatinib |
Healthy | University of California, San Francisco |
August 2011 | Phase 1 |
| NCT01238211 | Completed | Drug: Dasatinib Drug: Cytarabine |
Secondary Acute Myeloid Leukemia Acute Myeloid Leukemia |
National Cancer Institute (NCI) |
December 14, 2010 | Phase 2 |
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