Dasatinib Monohydrate (BMS354825; Sprycel)

Alias: Dasatinib; BMS-354825; Monohydrate; BMS354825; BMS 354825; Trade name: Sprycel

Cat No.:V0631 Purity: ≥98%

COA Product Data Instructions for use SDS

Dasatinib Monohydrate (BMS354825; Sprycel) Chemical Structure CAS No.: 863127-77-9
Product category: c-Kit

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Dasatinib Monohydrate (BMS354825; Sprycel):

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

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.

Biological Activity I Assay Protocols (From Reference)

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)

ln Vitro

Dasatinib is more efficient than imatinib at stopping the growth of Ba/F3 cells that express both Bcr-Abl mutants and the wild-type protein, with the exception of T315I. Comparatively speaking, dasatinib is roughly 325 times more potent than imatinib by two logs. All mutants except T315I and wild-type Abl kinase are potently inhibited by dasatinib within a specific range. Inhibiting autophosphorylation and substrate phosphorylation in a concentration-dependent manner, dasatinib directly targets both wild-type and mutant Abl kinase domains. When it comes to killing cells that express wild-type Bcr-Abl, dasatinib is 325 times more potent than imatinib.[1] The percentage of TgE bone marrow cell colonies dropped from 100% in untreated wells to 4.12% in wells treated with dasatinib. The percentage of colonies formed by WT and TgE bone marrow cells differs statistically significantly when dasatinib is present. Dasatinib can be used to target Lyn and/or c-Abl kinases, which will inhibit the promotion of B lymphocyte survival and proliferation that is brought about by the expression of LMP2A.[3] In a portion of thyroid cancer cells, dasatinib treatment causes Src signaling inhibition, growth inhibition, cell cycle arrest, and apoptosis. For a duration of three days, the C643, TPC1, BCPAP, and SW1736 cell lines are inhibited by approximately 50% at low nanomolar concentrations when treated with increasing doses of dasatinib (0.019 μM to 1.25 μM). However, the K1 cell line requires higher concentrations to effectively inhibit growth. The percentage of BCPAP, SW1736, and K1 cells in the G1 population increases by 9–22% when treated with 10 nM or 50 nM dasatinib, while the S phase cell percentage decreases by 7–18%.[4]

ln 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.

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.

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.

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.

References

[1]. Cancer Res . 2005 Jun 1;65(11):4500-5.

[2]. Blood . 2006 Jul 1;108(1):286-91.

[3]. Antiviral Res . 2012 Jul;95(1):49-56.

[3]. Clin Cancer Res . 2012 Jul 1;18(13):3580-91.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C22H28CLN7O3S
Molecular Weight	506.02
Exact Mass	487.16
Elemental Analysis	C, 52.22; H, 5.58; Cl, 7.01; N, 19.38; O, 9.49; S, 6.34
CAS #	863127-77-9
Related CAS #	Dasatinib;302962-49-8;Dasatinib hydrochloride;854001-07-3;Dasatinib-d8;1132093-70-9
Appearance	white solid powder
SMILES	CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.O
InChi Key	XHXFZZNHDVTMLI-UHFFFAOYSA-N
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
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
Synonyms	Dasatinib; BMS-354825; Monohydrate; BMS354825; BMS 354825; Trade name: Sprycel
HS Tariff Code	2934.99.9001
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)

Solubility Data

Solubility (In Vitro)

DMSO: ~21 mg/mL (~41.5 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

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

Biological Data

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.