Dasatinib monohydrate

SKU: orb1308590

Description

Dasatinib monohydrate

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 863127-77-9
• MW: 506.03
• Purity: 99.89%
• Formula: C₂₂H₂₈ClN₇O₃S
• SMILES: n1cc(sc1Nc1nc(nc(N2CCN(CC2)CCO)c1)C)C(=O)Nc1c(cccc1C)Cl.O
• Target: c-Kit,Apoptosis,Ephrin Receptor,Autophagy,Src,Bcr-Abl
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.95 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:123.75 mg/mL (244.55 mM)

Bioactivity

• Target IC50:
  Her2:710 nM|MEK:1700 nM|yes:0.5 nM|PDGFRβ:28 nM|lck:0.4 nM|FGFR1:880 nM|c-Kit (D816V):37 nM|Abl:0.6 nM|Src:0.8 nM|c-Kit (WT):79 nM|Her1:180 nM|p38:100 nM
• In Vivo:
  Dasatinib effectively inhibits wild-type Abl kinase and All its mutants (except T315I) by directly targeting All mutant Abl kinase domains and inhibiting substratee and autophosphorylation in a concentration dependent manner. Compared to Imatinib, Dasatinib demonstrates enhanced inhibitory efficacy o the proliferation of Ba/F3 cells expressing Bcr-Abl (wild-type and All mutants except T315I), exhibiting 325 time the potency against cells expressing wild-type Bcr-Abl. After treatment with Dasatinib the percentage o the TgE bone marrow cell colonies was reduced from 100% to 4.12%. There's a statistically significant difference in the colony formation percentage of WT and TgE bone marrow cells under Dasatinib treatment. It also inhibit the survival and proliferation of B lymphocytes induced by LMP2A expression. Additionally, Dasatinib suppresses Src signaling in certain thyroid cancer cells, inhibiting cell growth and inducing apoptosis and cell cycle arrest. A 3-day treatment with Dasatinib (0.019 μM~1.25 μM) inhibits approximately 50% growth in BCPAP, C643, SW1736, and TPC1 cell lines, with higher concentration required to inhibit K1 cell line growth. In BCPAP, SW1736, and K1 cells, Dasatinib (at 10 nM or 50 nM) increases G1 phase cells by 9-22% while correspondingly decreasing S phase cells by 7-18%.
• In Vitro:
  In TgE mice, Dasatinib specifically inhibit the formation of bone marrow B-cell colonies expressing LMP2A and reduces spleen size. Compared to the control Tg6/λ-MYC mice the Dasatinib-treated group exhibited significantly smaller spleen masses. Dasatinib also suppresses lymph node enlargement in MYC/LMP2A double transgenic mice and reverses splenomegaly. When tumor cells from LMP2A/MYC double transgenic mice are transplanted into Rag1KO mice, Dasatinib can revers the splenomegaly. Additionally, Dasatinib inhibits Lyn phosphorylation in B lymphoma cells expressing LMP2A.
• Cell Research:
  Ba/F3 cell lines are seeded in triplicate and incubated with escalating concentration of Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay. IC50 and IC90 Values are reported a the mean of three independent experiments done in quadruplicate the inhibitor concentration ranges are 0 nM to 32 nM (Dasatinib) the Dasatinib concentration range is extended to 200 nM for mutant T315I.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

WiDr, Src, prostate, K562, inhibit, PC3, orally, Inhibitor, EphA2, Ephrin Receptor, EphrinReceptor, Dasatinib, Dasatinib monohydrate, Dasatinib Monohydrate, colon, cKit, c-Kit (D816V), c-Kit (wt), CML, breast, active, Abl, antitumor, antiproliferative, Apoptosis, Autophagy, BMS 354825, BMS 354825 Monohydrate, BMS354825 Monohydrate, BMS-354825 Monohydrate, BMS354825, BMS-354825, BcrAbl, Bcr-Abl

Compound Identifiers

PubChem CID

11540687