Obatoclax mesilate
Obatoclax mesilate Basic information
- Product Name:
- Obatoclax mesilate
- Synonyms:
-
- OBATOCLAX MESYLATE
- 2-[2-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-1H-indole methanesulfonate
- Obatoclax mesilate
- 1H-Indole, 2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-, monomethanesulfonate
- Gx 15-070
- Gx 15-070ms
- Gx015-070
- Unii-39200fj43j
- CAS:
- 803712-79-0
- MF:
- C20H19N3O.CH4O3S
- MW:
- 413.49
- EINECS:
- 804-325-6
- Product Categories:
-
- Inhibitors
- Inhibitor
- INDOLE
- Mol File:
- 803712-79-0.mol
Obatoclax mesilate Chemical Properties
- 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.
Obatoclax mesilate Usage And Synthesis
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 Mesylate is a novel Bcl-2 homology domain-3 (BH3) mimetic.
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. |
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
Store at -20°C
References
[1] T NI CHONGHAILE A L. Mimicking the BH3 domain to kill cancer cells.[J]. Oncogene, 2008, 27 Suppl 1: S149-57. DOI:10.1038/onc.2009.52
[2] MARINA KONOPLEVA. Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax).[J]. Cancer research, 2008: 3413-3420. DOI:10.1158/0008-5472.can-07-1919
[3] GUAN WANG. Combination of chloroquine and GX15-070 (obatoclax) results in synergistic cytotoxicity against pancreatic cancer cells.[J]. Oncology reports, 2014, 32 6: 2789-2794. DOI:10.3892/or.2014.3525
[4] CHENGZHI XIE . Obatoclax potentiates the cytotoxic effect of cytarabine on acute myeloid leukemia cells by enhancing DNA damage[J]. Molecular Oncology, 2015, 9 2: Pages 409-421. DOI:10.1016/j.molonc.2014.09.008
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