BMS-354825 Monohydrate
Dasatinib monohydrate
CAS: 863127-77-9
Molecular Formula: C22H28ClN7O3S
BMS-354825 Monohydrate - Names and Identifiers
| Name | Dasatinib monohydrate |
| Synonyms | Dasatinib R dasatinib monohydrate Dasatinib monohydrate BMS-354825 Monohydrate n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2- N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide hydrate N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate Dasatinib monohydrate N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate |
| CAS | 863127-77-9 |
| EINECS | 638-874-6 |
| InChI | InChI=1/C22H27N7O2S2.H2O/c1-14-4-3-5-16(32)20(14)27-21(31)17-13-23-22(33-17)26-18-12-19(25-15(2)24-18)29-8-6-28(7-9-29)10-11-30;/h3-5,12-13,30,32H,6-11H2,1-2H3,(H,27,31)(H,23,24,25,26);1H2 |
BMS-354825 Monohydrate - Physico-chemical Properties
| Molecular Formula | C22H28ClN7O3S |
| Molar Mass | 506.02 |
| Melting Point | >223° (dec.) |
| Solubility | DMSO (Slightly, Sonicated), Methanol (Slightly, Sonicated) |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| In vitro study | Dasatinib inhibited the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants more effectively than imatinib, except for the T315I mutant. Dasatinib had a double-log (∼ 325-fold) increase in potency relative to imatinib. Dasatinib potently inhibited wild-type Abl kinase and a small range of all mutants except T315I. Dasatinib directly targets all mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Compared to imatinib, Dasatinib exhibited 325-fold potency against cells expressing wild-type Bcr-Abl. The percentage of TgE bone marrow cell colonies was 100% in untreated Wells and decreased to 4.12% in Dasatinib treated Wells. There was a statistically significant difference in the percentage of colonies formed by WT and TgE bone marrow cells in the presence of Dasatinib. Expression of LMP2A promotes B lymphocyte survival and proliferation, which can be inhibited by Dasatinib, which targets Lyn and/or c-Abl kinases. Dasatinib treatment inhibits Src signaling in a subset of thyroid cancer cells, reduces growth, and induces cell cycle arrest and apoptosis. Treatment with increasing doses of nanomolar Dasatinib (0.019 μM to 1.25 μm) for 3 days inhibited the growth of C643,TPC1,BCPAP, and SW1736 cell lines by approximately 50%, higher concentrations were required to inhibit the growth of the K1 cell line. Treatment with 10 nM or 50 nM Dasatinib resulted in a 9-22% increase in G1 phase cells and a corresponding 7-18% decrease in S phase cells in BCPAP ,SW1736 and K1 cells. |
| In vivo study | Dasatinib reverses splenomegaly in LMP2A/MYC double transgenic mice. In TgE mice, Dasatinib specifically prevents colony formation of lmp2a-expressing bone marrow B cells and reduces spleen size. Compared with the control group, the spleen mass was significantly reduced in the Tg6/λ-myc mice treated with Dasatinib. Dasatinib inhibits lymph node enlargement in LMP2A/MYC double transgenic mice. Dasatinib reversed splenomegaly in Rag1KO mice transplanted with tumor cells from LMP2A/MYC double transgenic mice. Dasatinib treatment inhibits phosphorylation of Lyn in lmp2a-expressing B lymphoid tumor cells. |
BMS-354825 Monohydrate - Risk and Safety
| HS Code | 29339900 |
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CAS: 863127-77-9
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