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Size | Price | Stock |
---|---|---|
5g | $180 | Check With Us |
10g | $280 | Check With Us |
20g | $420 | Check With Us |
Cat #: V0631 CAS #: 863127-77-9 Purity ≥ 98%
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.
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Molecular Weight (MW) | 506.02 |
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Molecular Formula | C22H28ClN7O3S |
CAS No. | 863127-77-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 21 mg/mL (41.5 mM)r |
Water: <1 mg/mLr | |
Ethanol: <1 mg/mL | |
Solubility In Vivo | 2% DMSO+30% PEG 300+dd H2O: 5 mg/mL |
SMILES Code | O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=C(C)C=CC=C4Cl.[H]O[H] |
Synonyms | Dasatinib; BMS-354825 Monohydrate; BMS354825; BMS 354825; Trade name: Sprycel. |
Protocol | In Vitro | 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. 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. |
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In Vivo | 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%. 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. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.9762 mL | 9.8810 mL | 19.7621 mL | 39.5241 mL |
5mM | 0.3952 mL | 1.9762 mL | 3.9524 mL | 7.9048 mL |
10mM | 0.1976 mL | 0.9881 mL | 1.9762 mL | 3.9524 mL |
20mM | 0.0988 mL | 0.4941 mL | 0.9881 mL | 1.9762 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.