Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

SHP099 [1801747-42-1]

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Cat# NB-64-23316-1mL

Size : 1mLx10mM(inDMSO)

Marca : Neo Biotech

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SHP099

(Synonyms: SHP099 free base, SHP-099, SHP 099) Copy Product Info

Synonyms: SHP099 free base, SHP-099, SHP 099

Catalog No. T3564 Copy Product Info

Purity: 99.4%

SHP099 is an oral, highly selective, allosteric SHP2 (PTPN11) inhibitor with an IC₅₀ of 70 nM. SHP099 inhibits tumor cell proliferation and survival by stabilizing the autoinhibitory conformation of SHP2 and blocking RAS-ERK signaling. SHP099 inhibits the growth of cancer cells, such as MV4-11 and TF-1 cells (IC₅₀ = 0.32 and 1.73 μM). SHP099 can be used in tumor research.

Cas No. 1801747-42-1

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.4%

Appearance:Solid

Color:White to Yellow

Product Introduction

SHP099 AI Summary

SHP099 exhibits bioactivity as an allosteric inhibitor of SHP2, including both wild type and E76A mutant forms, with IC50 values of 60.0 nM and 120.0 nM respectively. It shows significant antiproliferative activity against various human cancer cell lines, such as KYSE520, ASPC1, SW1990, BXPC-3, and MV4-11, with IC50 values ranging from 240.0 nM to 104800.0 nM. The compound also demonstrates antiviral activity against SARS-CoV-2, inhibiting virus-induced cytotoxicity in Caco-2 cells by 49.74% at 10 μM concentration after 48 hours. Additionally, SHP099 exhibits oral bioavailability in C57BL/6 mice at 5 mg/kg with a bioavailability percentage of 46.0% and high solubility exceeding 500,000.0 nM at pH 6.8. It also shows inhibition of HDAC6 and displays binding affinity to both wild type and mutant forms of SHP2, significantly inducing cell cycle arrest and enhancing antitumor immunity in mouse models. Overall, SHP099 presents as a promising multi-potent compound with potential applications in cancer therapy and antiviral treatment..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	SHP099 is an oral, highly selective, allosteric SHP2 (PTPN11) inhibitor with an IC₅₀ of 70 nM. SHP099 inhibits tumor cell proliferation and survival by stabilizing the autoinhibitory conformation of SHP2 and blocking RAS-ERK signaling. SHP099 inhibits the growth of cancer cells, such as MV4-11 and TF-1 cells (IC₅₀ = 0.32 and 1.73 μM). SHP099 can be used in tumor research.
Targets & IC50	SHP2 (E69K):0.416 μM, BaF3 cells:19.86 μM, Capan-2 cells:15.67 μM, SHP2:0.07 μM, pERK:0.250 μM, BXPC-3 cells:72.86 μM, SHP2 (D61Y):1.241 μM, SHP2A72V:1.968 μM, MV-4-11 cells:0.32 μM, TF-1 cell:1.73 μM, SHP2E76K:2.896 μM, 4T1 cells:119.3 μM, ASPC1 cells:64.04 μM
In vitro	Methods: RAW264.7 mouse macrophage cells were induced to differentiate into osteoclasts using RANKL (100 ng/mL). In some experiments, IL-6 (100 ng/mL) was added concurrently to simulate the post-injury inflammatory environment. Subsequently, 15 μM SHP099 was added and co-treated with the stimulant. The culture medium was changed every 2 days for a total duration of 5-6 days. Results: IL-6 enhanced RANKL-induced osteoclast differentiation and upregulated p-SHP2/p-TAK1 expression. SHP099 significantly reduced osteoclast numbers and downregulated mRNA and protein levels of osteoclast markers and proinflammatory cytokines. [1] Methods: Kmt2d KO LUSC cells were treated with SHP099 (1 μM) and/or afatinib (0.02 μM) for 7 days, followed by crystal violet staining to detect colony formation. Results: SHP099 significantly inhibited colony formation. [2]
In vivo	Methods: Bilateral proximal tibial drilling injuries were performed on 3-4-week-old C57BL/6J mice. The control group underwent no surgery. Intra-articular injection of SHP099 (30 mg/kg) was administered into the right knee as a single postoperative dose. Animals were euthanized for tissue collection 10 days post-surgery. Results: SHP099 treatment significantly suppressed tibial growth plate injury-induced gene upregulation, indicating its efficacy in inhibiting local osteoclastogenesis and inflammatory responses. [1] Methods: Kmt2d KO or Pten KO LUSC cells were injected via tail vein into B6-Albino mice. Tumor growth was monitored by MRI. When tumor volume reached 100–200 mm³, mice were randomly assigned to receive daily SHP099 (75 mg/kg) once daily, 5 days/week. Results: SHP099 monotherapy significantly inhibited tumor growth.[2]
Synonyms	SHP099 free base, SHP-099, SHP 099

Chemical Properties

Molecular Weight	352.26
Formula	C₁₆H₁₉Cl₂N₅
Cas No.	1801747-42-1
Smiles	CC1(N)CCN(CC1)c1cnc(c(N)n1)-c1cccc(Cl)c1Cl
Relative Density.	1.326 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 15.8 mg/mL (44.85 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.84 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8388 mL	14.1941 mL	28.3881 mL	141.9406 mL
5 mM	0.5678 mL	2.8388 mL	5.6776 mL	28.3881 mL
10 mM	0.2839 mL	1.4194 mL	2.8388 mL	14.1941 mL
20 mM	0.1419 mL	0.7097 mL	1.4194 mL	7.0970 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SHP-2SHP099PhosphatasePERKInhibitorinhibit

Related Tags: SHP099 chemical structure | SHP099 in vivo | SHP099 in vitro | SHP099 formula | SHP099 molecular weight