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CX-6258 Sale

(Synonyms: CX6258;CX 6258) 目录号 : GC13056

A pan-Pim kinase inhibitor

CX-6258 Chemical Structure

Cas No.:1202916-90-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,040.00
现货
5mg
¥662.00
现货
10mg
¥956.00
现货
25mg
¥2,016.00
现货
50mg
¥3,192.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Pim kinases (Provirus Integration site for Moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. This family of kinases is composed of three different isoforms (Pim-1, Pim-2, and Pim-3). The simultaneous inhibition of Pim-1, Pim-2, and Pim-3 kinases is emerging as a promising strategy for anticancer drug development. CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

In vitro: CX-6258 exhibited in vitro synergy with chemotherapeutics. The antiproliferative activity of CX-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. CX-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].

In vivo: CX-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia MV-4-11, and prostate adenocarcinoma PC3. The drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI. In addition, CX-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where Pim kinases had been shown to play an important role [1].

Clinical trial: No clinical data are available

Reference:
[1] Haddach M, Michaux J, Schwaebe MK, et al.  Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2011;3(2):135-9.

Chemical Properties

Cas No. 1202916-90-2 SDF
别名 CX6258;CX 6258
化学名 (E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one
Canonical SMILES CN1CCCN(C(C2=CC(C3=CC=C(/C=C4C(C=C(Cl)C=C5)=C5NC\4=O)O3)=CC=C2)=O)CC1
分子式 C26H24ClN3O3 分子量 461.94
溶解度 ≥ 11.15 mg/mL in DMSO, ≥ 2.575 mg/mL in Water with gentle warming 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1648 mL 10.8239 mL 21.6478 mL
5 mM 0.433 mL 2.1648 mL 4.3296 mL
10 mM 0.2165 mL 1.0824 mL 2.1648 mL
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