[CAS NO. 1357349-91-7]  SPP-86

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PRODUCTS SPECIFICATIONS [1357349-91-7]

Catalog
HY-110193
Brand
MCE
CAS
1357349-91-7

DESCRIPTION [1357349-91-7]

Overview

MDL-
Molecular Weight277.32
Molecular FormulaC16H15N5
SMILESCC(C)N1C2=NC=NC(N)=C2C(C#CC3=CC=CC=C3)=N1

For research use only. We do not sell to patients.

Summary

SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase , with an IC 50 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

Cell Line: Thyroid cancer derived cell lines expressing the RET/PTC1 rearrangement (TPC1), BRAF V600E (8505C) or RAS G13R (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.

Appearance

Solid


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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 360.59 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6059 mL 18.0297 mL 36.0594 mL
5 mM 0.7212 mL 3.6059 mL 7.2119 mL
10 mM 0.3606 mL 1.8030 mL 3.6059 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution

* All of the co-solvents are available by MCE.