SPP-86

Name: SPP-86
Brand: MedChemExpress
SKU: HY-110193
Rating: 4.5 (1 reviews)

Cat. No.: HY-110193 Purity: 99.62%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

SPP-86 Chemical Structure

CAS No. : 1357349-91-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 960	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE SPP-86

•Biomolecules. 2023 Dec 27, 14(1), 38.

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Biological Activity
Purity & Documentation
References
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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]. 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	> 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]
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	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	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	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]
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.

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.

Molecular Weight

277.32

Formula

C₁₆H₁₅N₅

CAS No.

1357349-91-7

Appearance

Solid

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

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)

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.62%

Select Batch:

Data Sheet (272 KB) SDS (392 KB)

COA (245 KB) LCMS (97 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]

Complete Stock Solution Preparation Table

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

SPP-86 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SPP-861357349-91-7SPP86SPP 86RETInhibitorinhibitorinhibit

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SPP-86

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SPP-86 Related Antibodies

1 Publications Citing Use of MCE SPP-86

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Complete Stock Solution Preparation Table

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