Gx 15-070ms
Obatoclax mesilate
CAS: 803712-79-0
Molecular Formula: C20H19N3O.CH4O3S
Gx 15-070ms - Names and Identifiers
| Name | Obatoclax mesilate |
| Synonyms | Gx 15-070 Gx015-070 Gx 15-070ms Unii-39200fj43j OBATOCLAX MESYLATE Obatoclax mesilate 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 |
| CAS | 803712-79-0 |
| EINECS | 804-325-6 |
| InChI | InChI=1/C20H19N3O.CH4O3S/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17;1-5(2,3)4/h4-11,21-22H,1-3H3;1H3,(H,2,3,4)/b19-10- |
Gx 15-070ms - Physico-chemical Properties
| Molecular Formula | C20H19N3O.CH4O3S |
| Molar Mass | 413.49 |
| Solubility | Soluble in DMSO (83 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (~2 mg/ml) |
| Appearance | solid |
| Color | Purple |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Use | A novel Bcl-2 homology domain-3 (BH3) mimetic. |
| In vitro study | 5 μm Obatoclax completely inhibited Mcl-1-involved Bak repair in SK-Mel5 cells and blocked anti-ABT-373-induced apoptosis of KB/Bcl-2 cells induced by Mcl-1. Obatoclax is a pseudobh3 that binds to many Bcl-2 family members, including Bcl-2, Bcl-xL, and Mcl-1. Obatoclax specifically displaces the Mcl-1 activating BH3 domain and subsequently causes Bak oligomerization and cytochrome C release-regulated apoptosis. Obatoclax is effective in cell lines that lack Bcl-xL or Bcl-xL low expression, and Obatoclax shows low cytotoxicity in all cell lines that strongly express Mcl-1, Bcl-2, and Bcl-xL. Obatoclax inhibits multiple myeloma (MM) cell lines such as KMS12PE, KMS18, MY5, etc., with an IC50 value of 52 to 1100nm. Inhibitory effects were also observed in the presence of an anticytotoxic agent IL-6 or IGF-1 at a concentration of 150 nmol. Obatoclax enhances the anti-Myeloma activity of melphalan, dexamethasone, or bortezomib. Obatoclax potentiates tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-regulated apoptosis. |
| In vivo study | Obatoclax was treated with 0.5 mg Obatoclax per kg of mouse body weight in SCID mice carrying human C33A uterine tumor, and the results showed strong anticancer activity. |
Gx 15-070ms - Introduction
Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist with a Ki of 0.22 μM, which can assist in inhibiting MCL-1-mediated anti-apoptosis effects. Phase 3.
Last Update：2022-10-16 17:29:04
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Product Name: Obatoclax Mesylate Visit Supplier Webpage Request for quotation
CAS: 803712-79-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 803712-79-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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