Cat. No.: HY-110193

SPP-86

Name: SPP-86
Brand: MedChemExpress
SKU: HY-110193
Price: 120.00 USD
Availability: InStock
Rating: 5 (2 reviews)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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. SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

Purity : 99.71%
CAS No.: 1357349-91-7
Formula: C₁₆H₁₅N₅
Molecular Weight:277.32

Storage:

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

SPP-86 Chemical Structure

CAS No.: 1357349-91-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Protocols (6)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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]. SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

IC50: 8 nM (RET)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	4500 nM Compound: 2	Growth inhibition of mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 48 hrs by MTT assay Growth inhibition of mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 48 hrs by MTT assay	[PMID: 26562217]
BaF3	IC₅₀	5020 nM Compound: 2	Growth inhibition of mouse BA/F3 cells expressing wild-type Bcr-Abl after 48 hrs by MTT assay Growth inhibition of mouse BA/F3 cells expressing wild-type Bcr-Abl after 48 hrs by MTT assay	[PMID: 26562217]
BaF3	GI₅₀	0.35 μM Compound: 7a	Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	0.61 μM Compound: 7a	Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	16.1 μM Compound: 7a	Cytotoxicity against mouse BAF3 cells after 48 hrs by MTT assay Cytotoxicity against mouse BAF3 cells after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	2.6 μM Compound: 7a	Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	5.43 μM Compound: 7a	Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	IC₅₀	>1000 nM Compound: 1	Antiproliferative activity against mouse BAF3 cells harboring CCDC6-RET fusion protein after 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring CCDC6-RET fusion protein after 72 hrs by CCK8 assay	[PMID: 28404375]
HCT-116	EC₅₀	2.4 μM Compound: 7a	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 22559926]
TPC1	EC₅₀	3.3 μM Compound: 7a	Antiproliferative activity against human TPC1 cells Antiproliferative activity against human TPC1 cells	[PMID: 22559926]
TT	GI₅₀	2.54 μM Compound: 7a	Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay	[PMID: 26652860]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

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]

View Protocol

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.

Chemical Information

CAS No. 1357349-91-7
Appearance Solid
Molecular Weight 277.32
Formula C₁₆H₁₅N₅
Color Off-white to light yellow
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

Publications (2)

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Drug Des Devel Ther

RET Inhibitor SPP86 Triggers Apoptosis and Activates the DNA Damage Response Through the Suppression of Autophagy and the PI3K/AKT Signaling Pathway in Melanoma Cells. [Abstract]

2025 Jan 7:19:67-82. PMID: 39803607
Biomolecules

GDF-15 Inhibits ADP-Induced Human Platelet Aggregation through the GFRAL/RET Signaling Complex. [Abstract]

2023 Dec 27;14(1):38. PMID: 38254638

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (360.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocols

All Signal Pathway Related Molecular Biology Cell Biology

Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of ³²P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Alao JP, et al. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer. 2014 Nov 20;14:853. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6059 mL	18.0297 mL	36.0594 mL	90.1486 mL
	5 mM	0.7212 mL	3.6059 mL	7.2119 mL	18.0297 mL
	10 mM	0.3606 mL	1.8030 mL	3.6059 mL	9.0149 mL
	15 mM	0.2404 mL	1.2020 mL	2.4040 mL	6.0099 mL
	20 mM	0.1803 mL	0.9015 mL	1.8030 mL	4.5074 mL
	25 mM	0.1442 mL	0.7212 mL	1.4424 mL	3.6059 mL
	30 mM	0.1202 mL	0.6010 mL	1.2020 mL	3.0050 mL
	40 mM	0.0901 mL	0.4507 mL	0.9015 mL	2.2537 mL
	50 mM	0.0721 mL	0.3606 mL	0.7212 mL	1.8030 mL
	60 mM	0.0601 mL	0.3005 mL	0.6010 mL	1.5025 mL
	80 mM	0.0451 mL	0.2254 mL	0.4507 mL	1.1269 mL
	100 mM	0.0361 mL	0.1803 mL	0.3606 mL	0.9015 mL

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SPP-86

Publications Citing Use of MedChemExpress (MCE) SPP-86