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> Dasatinib (hydrochloride) [854001-07-3]

Dasatinib (hydrochloride) [854001-07-3]

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Cat# HY-10181A-100mg

Size : 100mg

Brand : MedChemExpress

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Description

Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib hydrochloride also induces apoptosis and autophagy.

IC50 & Target[1]

Bcr-Abl

1.0 nM (IC50)

Src

0.5 nM (IC50)

lck

0.4 nM (IC50)

Yes

0.5 nM (IC50)

c-kit

5.0 nM (IC50)

PDGFRβ

28 nM (IC50)

p38

100 nM (IC50)

Her1

180 nM (IC50)

Her2

710 nM (IC50)

FGFR-1

880 nM (IC50)

MEK

1700 nM (IC50)

In Vitro

Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
? Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dasatinib hydrochloride Related Antibodies
In Vivo

Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
? Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing K562 xenografts
Dosage: 5 mg/kg and 50 mg/kg
Administration: Oral administration on a 5 day on and 2 day off schedule.
Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model: Sprague-Dawley Rats
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral and i.v.
Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.
Clinical Trial
Molecular Weight

524.47

Formula

C22H27Cl2N7O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C.12Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 15 mg/mL (28.60 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 10 mg/mL (19.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

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