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首页-小分子抑制剂&激动剂-Others-Other Targets-PCLX-001
PCLX-001

Chemical Structure : PCLX-001

CAS No.: 1215011-08-7

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PCLX-001 (Zelenirstat, PCLX001)

货号: PC-72143Not For Human Use, Lab Use Only.

PCLX-001 (Zelenirstat) is a potent, selective, orally bioavailable N-myristoyl-transferases (NMT1/2) inhibitor with IC50 of 5/8 nM, respectively.

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5 mg ￥2780 In stock
10 mg ￥4580 In stock
25 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PCLX-001 (Zelenirstat) is a potent, selective, orally bioavailable N-myristoyl-transferases (NMT1/2) inhibitor with IC50 of 5/8 nM, respectively.
PCLX-001 selectively kills hematological cancer cell lines in comparison to cancer cell lines of other origins.
PCLX-001 selectively inhibits myristoylation in vitro and induces apoptosis in lymphoma cell lines, does not inhibit any of the 468 human kinases at 10 uM.
PCLX-001 reduces SFK levels and BCR downstream signaling.
PCLX-001 attenuates BCR downstream signaling events in BL2 lymphoma cells.
PCLX-001 selectively kills hematological cancer cells (IC50=0.166 uM) relative to benign lymphocytes in comparison to dasatinib and ibrutinib.
PCLX-001 reduces tumor volumes and leads to complete tumor regression in B-cell lymphoma xenograft models.
PCLX-001 can efficiently target breast cancer by reducing the viability of numerous breast cancer cell lines in vitro and cause disease regression in vivo in an established murine xenograft breast cancer model.

物理化学性质&存储条件

分子量 537.504
分子式 C24H30Cl2N6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2,6-Dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)-1H-pyrazol-4-yl]-4-[2-(1-piperazinyl)-4-pyridinyl]benzenesulfonamide

参考文献

1. Beauchamp E, et al. Nat Commun. 2020 Oct 22;11(1):5348.

2. Mackey JR, Lai J,et al. Breast Cancer Res Treat. 2021 Feb;186(1):79-87.

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