1. Protein Tyrosine Kinase/RTK
  2. RET
  3. SPP-86

SPP-86 

目录号: HY-110193 纯度: >99.0%
产品使用指南

SPP-86 是一种选择性的 RET 酪氨酸激酶的有效抑制剂,其 IC50 值为 8 nM。SPP-86 抑制 MCF7 细胞中 RET 诱导激活的 PI3K/Akt 和 MAPK 信号通路,也能抑制 RET 诱导的 ERα 磷酸化。

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SPP-86 Chemical Structure

SPP-86 Chemical Structure

CAS No. : 1357349-91-7

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Description

SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells[1].

IC50 & Target

IC50: 8 nM (RET)[1].

In Vitro

SPP86 (0-10 μM) inhibits MAPK signaling and proliferation in RET/PTC1 expressing TPC1 but not 8505C or C643 cells[1].
SPP86 (0-10 μM) inhibits RET- induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling and estrogen receptorα (ERα) phosphorylation in MCF7 cells[1].

Western Blot Analysis[1]

Cell Line: Thyroid cancer derived cell lines expressing the RET/PTC1 rearrangement (TPC1), BRAFV600E (8505C) or RASG13R (C643) mutations.
Concentration: 0-10 μM.
Incubation Time: 90 min.
Result: Inhibited RET- induced ERK1/2 phosphorylation in thyroid cancer cell lines.

Western Blot Analysis[1]

Cell Line: MCF7 cells (human breast cancer).
Concentration: 0-10 μM.
Incubation Time: 30 min.
Result: Inhibited RET- induced ERα phosphorylation and proliferation in MCF7 cells.
Molecular Weight

277.32

Formula

C₁₆H₁₅N₅

CAS No.

1357349-91-7

SMILES

CC(C)N1C2=NC=NC(N)=C2C(C#CC3=CC=CC=C3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

SPP-86SPP86SPP 86RETInhibitorinhibitorinhibit

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产品名称:
SPP-86
目录号:
HY-110193
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