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Chemical Structure : Pelcitoclax
Catalog No.: PC-49798Not For Human Use, Lab Use Only.
Pelcitoclax (APG-1252, BM-1252) is a potent dual specific Bcl-2/Bcl-xL inhibitor with Ki of < 1 nM, shows potent antitumor effects with minimal platelet toxicity.
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Pelcitoclax (APG-1252, BM-1252) is a potent dual specific Bcl-2/Bcl-xL inhibitor with Ki of < 1 nM, shows potent antitumor effects with minimal platelet toxicity.
Pelcitoclax (APG-1252, BM-1252) changes to its reactive metabolite, named APG-1252-M1, in vivo can disrupt the anti-apoptotic function of these proteins with potent antitumor effects.
APG-1252 is >10- times less active than APG-1252-M1 in cell growth assay in a panel of small cell lung cancer (SCLC) cell lines.
APG-1252-M1 induces Bax/Bak-dependent apoptosis in MEF/MCL1−/− model cell line.
APG-1252 is >30-times less effective in platelet killing than BM-1252-M1 in animals. APG-1252-M1 exerts nanomolar single agent activity in a small subset of colorectal cancer (CRC) cell lines and synergizes with MEK inhibitor trametinib in a large subset of CRC cell lines.
APG-1252 plus gemcitabine exhibited even remarkable antitumor activity in vivo, has synergistic anticancer activities against advanced nasopharyngeal carcinoma (NPC).
| M.Wt | 1281.84 | |
| Formula | C57H66ClF4N6O11PS4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yi H, et al. Cancer Med. 2020 Jun;9(12):4197-4206.
2. Luo F, et al. Cell Death Dis. 2021 Aug 5;12(8):772.
3. Bai L, et al. Eur J Cancer. 2014;50:109–10.
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