| Identification | Back Directory | [Name]
Obatoclax mesilate | [CAS]
803712-79-0 | [Synonyms]
CS-393
Gx 15-070
Gx015-070
Gx 15-070ms
Unii-39200fj43j
OBATOCLAX MESYLATE
Obatoclax mesilate
Obatoclax (GX15-070)
Obatoclax mesylate, >=98%
GX-15070, Obatoclax Mesylate
Obatoclax mesilate USP/EP/BP
Obatoclax Mesylate (GX15-070)
Obatoclax mesylate(GX 015070)
Obatoclax, Methanesulfonate Salt
2-(2-((3,5-Dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-1H-indole methanesulfo
(Z)-2-(5-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-4-methoxy-5H-pyrrol-2-yl)-1H-indole mesylate
2-(2-((3,5-Dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-1H-indole methanesulfonat
2-[2-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-1H-indole methanesulfonate
1H-Indole, 2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-, monomethanesulfonate | [EINECS(EC#)]
804-325-6 | [Molecular Formula]
C20H19N3O.CH4O3S | [MDL Number]
MFCD18074508 | [MOL File]
803712-79-0.mol | [Molecular Weight]
413.49 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 5 mg/ml). | [form ]
solid | [color ]
Purple | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
Obatoclax (803712-79-0) is a novel Bcl-2 homology domain-3 (BH3) mimetic.1?Inhibits primary acute myeloid leukemia (AML) progenitor cell proliferation (IC50=0.18 μM) and induces apoptosis in primary AML cells (IC50= 3.6 μM).2?Obatoclax synergizes with other agents such as chloroquine3?and cytarabine4?in cytotoxicity against a variety of cancer cells. | [Chemical Properties]
Red powder | [Uses]
Obatoclax (GX15-070) is an inhibitor of Bcl-2 with Ki of 0.22 μM. | [in vivo]
Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner[4].
| Animal Model: | 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors[4] | | Dosage: | 1.15, 2.5, 5 mg/kg | | Administration: | Intravenously injected (through lateral tail vein); five consecutive days (i.e. 5 injections) | | Result: | Exhibited potent antitumor activity in xenograft mouse models in a dose-dependent manner.
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| [IC 50]
Bcl-2: 220 nM (Ki); Mcl-1: 1-7 μM (Ki); Bcl-xL: 1-7 μM (Ki); Bcl-W: 1-7 μM (Ki); Bcl-B: 1-7 μM (Ki) | [storage]
4°C, protect from light | [References]
1) Chonghaile and Letai (2008),?Mimicking the BH3 domain to kill cancer cells; Oncogene,?27?S149
2) Konopleva?et al. (2008),?Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax); Cancer Res.,?68?3413
3) Wang?et al. (2014),?Combination of chloroquine and GX15-070 (obatoclax) results in synergistic cytotoxicity against pancreatic cancer cells; Oncol. Rep.,?32?2789
4) Xie?et al. (2015),?Obatoclax potentiates the cytotoxic effect of cytarabine on acute myeloid leukemia cells by enhancing DNA damage; Mol. Oncol.,?9?409 |
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