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Obatoclax Mesylate

Cat. No. M3757
Obatoclax Mesylate Structure

GX15-070, Obatoclax

Size Price Availability Quantity
2mg USD 55  USD55 In stock
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 250  USD250 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon. Obatoclax prevents the interaction of these pro-survival proteins with Bax or Bak, thereby inducing apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3. Obstoclax also induces autophagy in mouse embryo fibroblasts and in HeLa cells.This compound inhibits the growth of cancer cell lines and primary cancer isolates. Obatoclax enhances cytarabine-induced apoptosis by enhancing DNA DSBs. This novel mechanism provides compelling evidence for the clinical use of BH3 mimetics in combination with DNA-damaging agents in AML and possibly a broader range of malignancies.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 413.49
Formula C20H19N3O.CH4O3S
CAS Number 803712-79-0
Purity >98%
Solubility DMSO ≥80 mg/mL
Storage at -20°C

[1] Wang G, et al. Oncol Rep. Combination of chloroquine and GX15-070 (obatoclax) results in synergistic cytotoxicity against pancreatic cancer cells.

[2] Xie C, et al. Mol Oncol. Obatoclax potentiates the cytotoxic effect of cytarabine on acute myeloid leukemia cells by enhancing DNA damage.

[3] Kim PS, et al. Oncoimmunology. Potential utility of the pan-Bcl-2 inhibitor GX15-070 (obatoclax) in cancer immunotherapy.

[4] Champa D, et al. Endocr Relat Cancer. Obatoclax overcomes resistance to cell death in aggressive thyroid carcinomas by countering Bcl2a1 and Mcl1 overexpression.

[5] Nguyen M, et al. Proc Natl Acad Sci U S A. Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.

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Keywords: Obatoclax Mesylate, GX15-070, Obatoclax supplier, Bcl-2, inhibitors

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