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Purity: ≥98%
Dasatinib (formerly BMS-354825; trade name Sprycel), an approved anticancer drug, is an orally bioavailable and multi-targeted kinase inhibitorof Abl, Src and c-Kit with potential anticancer activity. In cell-free assays, it inhibits the aforementioned kinases with IC50 values of less than 1 nM, 0.8 nM, and 79 nM, respectively. In 2006, the FDA approved dasatinib for the treatment of acute lymphoblastic leukemia (ALL) and chronic myelogenous leukemia (CML), particularly in patients who have the Philadelphia chromosome.
| Targets |
Bcr-Abl (IC50 = 1.0 nM); Src (IC50 = 0.5 nM); lck (IC50 = 0.4 nM); yes (IC50 = 0.5 nM); c-kit (IC50 = 5.0 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 |
Glutathione S-transferase (GST)-Abl fusion proteins, both wild-type and mutant (c-Abl amino acids 220-498), are used in kinase experiments. Prior to usage, the GST-Abl fusion proteins are liberated from glutathione-Sepharose beads; 5 μM of ATP is present. Tyrosine phosphatase (LAR) treatment is applied to GST-Abl kinase domain fusion proteins just prior to their utilization in kinase autophosphorylation and in vitro peptide substrate phosphorylation techniques. Sodium vanadate (1 mM) is added to inactivate LAR phosphatase following a 30-minute incubation period at 30°C. Phosphotyrosine-specific antibody 4G10 is commonly used in immunoblot analysis to confirm complete (>95%) dephosphorylation of tyrosine residues, while c-Abl antibody CST 2862 is used to confirm equal loading of GST-Abl kinase.The analysis compares untreated GST-Abl kinase to dephosphorylated GST-Abl kinase. For mutant T315I, dasatinib is now available at a concentration range of 1,000 nM. For the in vitro peptide substrate phosphorylation assays, the same inhibitor concentrations are utilized. GST-Src kinase and GST-Lyn kinase are tested against the three inhibitors within these same concentration ranges.
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| Cell Assay |
Ba/F3 cell lines are cultured in triplicate and exposed to increasing doses of dasatinib for a duration of 72 hours. The methanethiosulfonate-based viability assay is used to quantify proliferation. The mean of three separate, quadruplicate experiments is used to calculate the IC50 and IC90 values. The concentration ranges for the inhibitor (dasatinib) are 0 nM to 32 nM. For mutant T315I, the dasatinib concentration range is increased to 200 nM.
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| Animal Protocol |
EμLMP2A (TgE and Tg6 strains), MYC (λ-MYC), and LMP2A/λ-MYC double transgenic mice (Tg6/λ-MYC)
30 mg/kg Administered via i.p. |
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| References | ||
| Additional Infomation |
Dasatinib monohydrate is a hydrate that is the monohydrate of dasatinib. It is used for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It contains a dasatinib (anhydrous).
Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with a variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes. A pyrimidine and thiazole derived ANTINEOPLASTIC AGENT and PROTEIN KINASE INHIBITOR of BCR-ABL KINASE. It is used in the treatment of patients with CHRONIC MYELOID LEUKEMIA who are resistant or intolerant to IMATINIB. See also: Dasatinib (annotation moved to). |
| Molecular Formula |
C22H28CLN7O3S
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|---|---|
| Molecular Weight |
506.02
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| Exact Mass |
505.166
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| Elemental Analysis |
C, 52.22; H, 5.58; Cl, 7.01; N, 19.38; O, 9.49; S, 6.34
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| CAS # |
863127-77-9
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| Related CAS # |
Dasatinib;302962-49-8;Dasatinib hydrochloride;854001-07-3;Dasatinib-d8;1132093-70-9
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| PubChem CID |
11540687
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| Appearance |
White solid powder
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| Density |
1.408 g/cm3
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| Melting Point |
97-99 °C(lit.)
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| LogP |
3.398
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
642
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CN=C(NC2C=C(N3CCN(CCO)CC3)N=C(C)N=2)S1)NC1C(C)=CC=CC=1Cl.O
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| InChi Key |
XHXFZZNHDVTMLI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26ClN7O2S.H2O/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);1H2
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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;hydrate
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| Synonyms |
Dasatinib; BMS-354825 Monohydrate; BMS354825; 863127-77-9; Dasatinib hydrate; Dasatinib (monohydrate); BMS 35482503; dasatinib.H2O; Dasatinib [USAN]; RBZ1571X5H; BMS 354825; Trade name: Sprycel
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| HS Tariff Code |
2934.99.9001
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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: ≥ 2.5 mg/mL (4.94 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 25.0 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: 2% DMSO+30% PEG 300+dd H2O: 5 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9762 mL | 9.8810 mL | 19.7621 mL | |
| 5 mM | 0.3952 mL | 1.9762 mL | 3.9524 mL | |
| 10 mM | 0.1976 mL | 0.9881 mL | 1.9762 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 |
| NCT02689440 | Active Rrecruiting |
Drug: Dasatinib Drug: Venetoclax |
Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive |
M.D. Anderson Cancer Center | February 19, 2016 | Phase 2 |
| NCT00070499 | Active Rrecruiting |
Drug: Dasatinib Drug: Imatinib Mesylate |
Chronic Myeloid Leukemia, BCR-ABL1 Positive |
National Cancer Institute (NCI) |
August 15, 2004 | Phase 2 |
| NCT04164069 | Active Rrecruiting |
Drug: Dasatinib Drug: Fluorouracil |
Gastric Cancer Bile Duct Cancer |
Anne Noonan | September 2, 2020 | Phase 1 |
| NCT02143414 | Active Rrecruiting |
Procedure: Biopsy Drug: Dasatinib |
Acute Lymphoblastic Leukemia B Acute Lymphoblastic Leukemia |
National Cancer Institute (NCI) |
June 30, 2015 | Phase 2 |
| NCT01660971 | Active Rrecruiting |
Drug: Dasatinib Drug: Erlotinib Hydrochloride |
Recurrent Pancreatic Carcinoma Stage III Pancreatic Cancer AJCC v6 and v7 |
National Cancer Institute (NCI) |
July 30, 2012 | Phase 1 |
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Dasatinib inhibits splenomegaly and lymphadenopathy in Tg6/λ-MYC mice.Antiviral Res.2012 Jul;95(1):49-56. |
Dasatinib inhibits colony formation by bone marrow cells from LMP2A transgenic (TgE) mice.Antiviral Res.2012 Jul;95(1):49-56. |
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