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Merck
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Key Documents

SML0762

Sigma-Aldrich

Enzastaurin

≥98% (HPLC)

别名:

3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione, D04014, LY-317615, LY317615

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About This Item

经验公式(希尔记法):
C32H29N5O2
分子量:
515.60
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

, light orange to dark orange-red

溶解度

DMSO: 10 mg/mL, clear (warmed)

儲存溫度

−20°C

InChI

1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)

InChI 密鑰

AXRCEOKUDYDWLF-UHFFFAOYSA-N

應用

Enzastaurin has been used in splicing analysis to study its effects on splicing of a mutated exon.

生化/生理作用

Enzastaurin is a potent and PKCβ preferring inhibitor. Also, Enzastaurin inhibits AKT and GSK3β. Enzastaurin acts as anti-angiogenic and antineoplastic agent.
It is an orally administered drug. It can induce apoptosis, inhibit angiogenesis and proliferation of cells. Enzastaurin can be used for the treatment of haematological cancers.

特點和優勢

This compound is featured on the GSK-3, PKB/Akt and PKC pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Acute Tox. 4 Oral - Aquatic Chronic 4

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Enzastaurin: A lesson in drug development.
Bourhill T
Critical Reviews in Oncology/Hematology (2017)
Staurosporine allows dystrophin expression by skipping of nonsense-encoding exon
Atsushi N
Brain & Development (2016)
Shannon M White et al.
Developmental cell, 49(3), 425-443 (2019-05-08)
Merlin/NF2 is a bona fide tumor suppressor whose mutations underlie inherited tumor syndrome neurofibromatosis type 2 (NF2), as well as various sporadic cancers including kidney cancer. Multiple Merlin/NF2 effector pathways including the Hippo-YAP/TAZ pathway have been identified. However, the molecular

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