Dasatinib

SKU: orb1308592

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Description

Dasatinib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	302962-49-8
MW	488.01
Purity	99.89%
Formula	C₂₂H₂₆ClN₇O₂S
SMILES	N(C1=CC(N2CCN(CCO)CC2)=NC(C)=N1)C=3SC(C(NC4=C(C)C=CC=C4Cl)=O)=CN3
Target	Bcr-Abl,c-Kit,Apoptosis,Autophagy,Src
Solubility	DMSO:262.5 mg/mL (537.9 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:9.1 mg/mL (18.65 mM)

Bioactivity

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Target IC50	Abl:0.6 nM (cell free)\|lck:0.4 nM\|FGFR1:880 nM\|c-Kit (D816V):37 nM (cell free)\|Her2:710 nM\|MEK:1700 nM\|yes:0.5 nM\|PDGFRβ:28 nM\|Src:0.8 nM (cell free)\|c-Kit (WT):79 nM (cell free)\|p38:100 nM\|Her1:180 nM\|p210 (BCR-ABL):1.0 nM Read more...
In Vivo	METHODS: To tes the antitumor activity in vivo Dasatinib (50 mg/kg in 80 mmol/L sodium citrate buffer, pH 3.0) was administered orally to athymic nude mice harboring human thyroid carcinoma tumors of BCPAP or 8505C, five days per week for 20 days. Results: Dasatinib significantly inhibited BCPAP tumors in situ, with final tumor volume suppressed by more than 90%. Dasatinib treatment did not significantly inhibi the growth of 8505C-derived tumors at any time point. METHODS: To investigat the effects on neuroinflammation, Dasatinib (20 mg/kg in 4%DMSO+30%PEG+5%Tween 80) was administered intraperitoneally or orally to C57BL-/- mice once daily for four days, followed by intraperitoneal injection of LPS (10 mg/kg) to induce neuroinflammatory responses in vivo Results: Intraperitoneal injection and oral administration of Dasatinib inhibited LPS-induced activation of microglia/astrocytes, pro-inflammatory cytokine levels, and neutrophil rolling in the brains of wild-type mice. Read more...
In Vitro	METHODS: Eight thyroid cancer cells were treated with Dasatinib (0.019-1.25 μMol/L) for 3 days, and cell proliferation was detected by SRB. Results the IC50 of Dasatinib on C643, TPC1, BCPAP, SW1736, K1, 8505C, HTh74 and HTh7 cells were 0.09, 0.03, 0.04, 0.08, 0.4, 2.7, >5 and 1.6 μMol/L, respectively METHODS: Human lung cancer cells NCI-H1975 and NCI-H1650 were treated with Dasatinib (2.5-20 μM) for 48 h. Apoptosis was detected by Flow Cytometry. Results: Dasatinib induced apoptosis in NCI-H1975 and NCI-H1650 cells at 10 and 20 μM. Read more...
Cell Research	Ba/F3 cell lines were plated in triplicate and incubated with escalating concentration of imatinib, AMN107, or BMS-354825 for 72 hours. Proliferation was 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 for IC50 and IC90 determinations were 0 to 2,000 nMol/L (imatinib and AMN107) or 0 to 32 nMol/L (BMS-354825) the imatinib concentration range was extended to 6,400 nMol/L for mutants with IC50 >2,000 nMol/L the BMS-354825 concentration range was extended to 200 nMol/L for mutant T315I. Read more...
Animal Research	For in vivo studies, dasatinib (50 mg/kg) was prepared for daily oral gavage (5 d/wk) in 80 mmol/L sodium citrate buffer, pH 3.0. Fo the orthotopic murine model, mice were andomized on day 10 based on bioluminescence activity to receive drug or Vehicle. in the metastatic murine model, mice received dasatinib or Vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following andomization (posttreatment) . Read more...

Storage & Handling

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Storage	store at low temperature,keep away from moisture \| 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

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

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Compound Identifiers

PubChem CID

3062316 ↗

Key Properties

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No computed properties available.

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Dasatinib (orb1308592)

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Applications:	FC, WB
Reactivity:	Human, Mouse
Species/Host:	Rabbit
Clonality:	Monoclonal
Conjugation:	Unconjugated

Applications:	FC, WB
Reactivity:	Human
Species/Host:	Rabbit
Clonality:	Monoclonal
Conjugation:	Unconjugated

MW:	1269.9
Formula:	C₆₅H₇₇ClN₁₂O₁₁S

CAS Number:	3079237-53-6
MW:	1188.69
Formula:	C₄₁H₅₄ClN₉O₂₀S₅

MW:	1042.6
Formula:	C₅₅H₅₂ClN₁₃O₅S

Dasatinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Dasatinib (orb1308592)

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