SHP099

Name: SHP099
Brand: MedChemExpress
SKU: HY-100388
Rating: 5.0 (64 reviews)

Cat. No.: HY-100388 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SHP099 is an allosteric SHP2 inhibitor, with IC₅₀s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2^D61Y, SHP2E69K, SHP2^A72V, SHP2^E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC₅₀: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth.

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

SHP099 Chemical Structure

CAS No. : 1801747-42-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 70	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 70	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 64 publication(s) in Google Scholar

Other Forms of SHP099:

SHP099 monohydrochloride In-stock
SHP099 hydrochloride Get quote

60 Publications Citing Use of MCE SHP099

: SHP099 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Oct;8(10):1237-1249. [Abstract]; Immunoblots of whole cell lysates or GST-RBD-precipitated (RAS-GTP, KRASGTP and NRAS-GTP) lysates from PDAC cells treated with DMSO, SHP099 10 μM, AZD6244 1 μM, or both drugs for the times indicated.

: SHP099 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 1;10(1):1473. [Abstract]; SHP099 inhibits IRS1-AP2 interaction in primary hepatocytes.

: SHP099 purchased from MedChemExpress. Usage Cited in: Hepatology. 2018 Jul;68(1):333-348. [Abstract]; Primary human HSCs are treated with SHP099 for 1 hour. PDGF-BB is added and cells are cultured for 12 additional hours. Whole cell lysates and EVs are examined by WB (n=6).

: SHP099 purchased from MedChemExpress. Usage Cited in: Open Biol. 2017 May;7(5). pii: 170066. [Abstract]; Comparing the effects of SHP2 degradation and allosteric inhibition on Ras/MAPK signalling. (a) Human U2OS, A549, K-562 and MDA-MB-468 cells are treated with DMSO control or 1, 5 and 10 µM SHP099 for 2 h prior to lysis. Extracts (10 µg protein) are resolved by SDS-PAGE and transferred to nitrocellulose membranes, which are subjected to western blotting with the indicated antibodies. (b) Uninfected U2OS cells (WT) or cells infected with retroviruses encoding VHL, aCS3 and VHL-aCS3 are treated wit

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Biological Activity
Protocol
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References
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Description

IC₅₀ & Target

IC50: 70 nM (SHP2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	119.3 μM Compound: SHP099	Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
ASPC1	IC₅₀	64.04 μM Compound: SHP099	Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
BaF3	IC₅₀	19.86 μM Compound: SHP-099	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33582386]
BXPC-3	IC₅₀	72.86 μM Compound: SHP099	Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
Capan-2	IC₅₀	15.67 μM Compound: SHP-099	Cytotoxicity against human Capan-2 cells harbouring K-ras mutant assessed as reduction in cell viability incubated for 144 hrs Cytotoxicity against human Capan-2 cells harbouring K-ras mutant assessed as reduction in cell viability incubated for 144 hrs	[PMID: 33582386]
Detroit 562	IC₅₀	6.47 μM Compound: 2; SHP099	Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay	[PMID: 30688459]
KYSE-520 cell line	IC₅₀	1.4 μM Compound: 1	Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability measured after 5 days by Celltiter-Glo assay Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability measured after 5 days by Celltiter-Glo assay	[PMID: 27347692]
KYSE-520 cell line	IC₅₀	1.4 μM Compound: 2; SHP099	Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay	[PMID: 30688459]
KYSE-520 cell line	IC₅₀	13.22 μM Compound: SHP099	Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
KYSE-520 cell line	IC₅₀	18.2 μM Compound: 1; SHP099	Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay	[PMID: 32437146]
MDA-MB-468	IC₅₀	29.9 μM Compound: SHP099	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay	[PMID: 31784318]
MDA-MB-468	IC₅₀	49.6 μM Compound: SHP099	Antiproliferative activity against human MDA-MB-468 3D spheroids assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay Antiproliferative activity against human MDA-MB-468 3D spheroids assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay	[PMID: 31784318]
MOLM-14	IC₅₀	0.9 μM Compound: SHP099	Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo luminescence assay Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo luminescence assay	[PMID: 29089257]
MV4-11	IC₅₀	0.24 μM Compound: SHP099	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of SAHA by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of SAHA by CCK-8 assay	[PMID: 36097406]
MV4-11	IC₅₀	0.475 nM Compound: 1; SHP099	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 33780898]
MV4-11	IC₅₀	0.572 μM Compound: 1; SHP099	Cytotoxicity against human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay Cytotoxicity against human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay	[PMID: 33780898]
MV4-11	IC₅₀	0.803 μM Compound: 1; SHP099	Cytotoxicity against CRBN knock out human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay Cytotoxicity against CRBN knock out human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay	[PMID: 33780898]
MV4-11	IC₅₀	1 μM Compound: 1; SHP099	Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay	[PMID: 32437146]
MV4-11	IC₅₀	1.75 μM Compound: SHP099	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
SW1990	IC₅₀	104.8 μM Compound: SHP099	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]

In Vitro

The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC₅₀ of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells^[1]. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells^[2].

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

In Vivo

After a single dose of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg^[1].

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

Molecular Weight

352.26

Formula

C₁₆H₁₉Cl₂N₅

CAS No.

1801747-42-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=NC(N2CCC(C)(N)CC2)=CN=C1C3=CC=CC(Cl)=C3Cl

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 : 12 mg/mL (34.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8388 mL	14.1941 mL	28.3881 mL
5 mM	0.5678 mL	2.8388 mL	5.6776 mL
10 mM	0.2839 mL	1.4194 mL	2.8388 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: ≥ 1.2 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.0 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: ≥ 1.2 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.0 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: ≥ 1.2 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.2 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 (12.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 0.67 mg/mL (1.90 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.67 mg/mL (1.90 mM); Clear solution
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.13 mg/mL (0.37 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (28.39 mM); Suspended solution; Need ultrasonic

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: 99.80%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52. [Content Brief]

[2]. Sun X, et al. Selective inhibition of leukemia-associated SHP2E69K mutant by the allosteric SHP2 inhibitor SHP099. Leukemia. 2018 May;32(5):1246-1249. [Content Brief]

Kinase Assay ^[1]	The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52. [Content Brief] [2]. Sun X, et al. Selective inhibition of leukemia-associated SHP2E69K mutant by the allosteric SHP2 inhibitor SHP099. Leukemia. 2018 May;32(5):1246-1249. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8388 mL	14.1941 mL	28.3881 mL	70.9703 mL
	5 mM	0.5678 mL	2.8388 mL	5.6776 mL	14.1941 mL
	10 mM	0.2839 mL	1.4194 mL	2.8388 mL	7.0970 mL
	15 mM	0.1893 mL	0.9463 mL	1.8925 mL	4.7314 mL
	20 mM	0.1419 mL	0.7097 mL	1.4194 mL	3.5485 mL
	25 mM	0.1136 mL	0.5678 mL	1.1355 mL	2.8388 mL
	30 mM	0.0946 mL	0.4731 mL	0.9463 mL	2.3657 mL

SHP099 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:

SHP0991801747-42-1SHP 099SHP-099SHP2PhosphataseSrc homology phosphatase 2PTPN11RAS-ERK signalingtumorallostericMV4-11TF-1Inhibitorinhibitorinhibit

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SHP099

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60 Publications Citing Use of MCE SHP099

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