SHP099 monohydrochloride
Based on 76 publication(s) in Google Scholar
SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 2200214-93-1
- Formula: C16H20Cl3N5
- Molecular Weight:388.72
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) SHP099 monohydrochloride
More- Signal Transduct Target Ther. 2022 Sep 12;7(1):317. [Abstract]
- Cancer Discov. 2018 Oct;8(10):1237-1249. [Abstract]
- Nat Immunol. 2021 Nov;22(11):1391-1402. [Abstract]
- Cancer Res. 2021 Jun 15;81(12):3215-3228. [Abstract]
- Cancer Res. 2020 Aug 15;80(16):3413-3423. [Abstract]
- Nat Commun. 2023 Apr 6;14(1):1933. [Abstract]
- Nat Commun. 2019 Apr 1;10(1):1473. [Abstract]
- Nat Commun. 2018 Oct 30;9(1):4507. [Abstract]
- Hepatology. 2020 Jul;72(1):155-168. [Abstract]
- Hepatology. 2018 Jul;68(1):333-348. [Abstract]
- Exp Mol Med. 2020 Jun;52(6):911-920. [Abstract]
- ACS Nano. 2023 Aug 22;17(16):16056-16068. [Abstract]
- Mol Cell. 2026 Feb 19;86(4):674-692.e10. [Abstract]
- Mol Cell. 2021 Oct 7;81(19):4076-4090.e8. [Abstract]
- Nat Chem Biol. 2025 Aug;21(8):1226-1237. [Abstract]
- Sci Transl Med. 2025 May 7;17(797):eads2694. [Abstract]
- Theranostics. 2021 Jan 1;11(2):555-566. [Abstract]
- Acta Pharm Sin B. 2024 Jun;14(6):2598-2612. [Abstract]
- Acta Pharm Sin B. 2022 Jul;12(7):3073-3084. [Abstract]
- Acta Pharm Sin B. 2022 Jan;12(1):149-166. [Abstract]
- J Clin Invest. 2026 May 1;136(9):e199303. [Abstract]
- MedComm (2020). 2022 Mar 4;3(1):e120. [Abstract]
- Neuro Oncol. 2025 Mar 6:noaf057. [Abstract]
- Neuro Oncol. 2019 Nov 4;21(11):1423-1435. [Abstract]
- J Control Release. 2025 Aug 10:384:113889. [Abstract]
- J Exp Med. 2022 Apr 4;219(4):e20210739. [Abstract]
- Nano Today. 2025 Apr.
- NPJ Precis Oncol. 2024 Jul 16;8(1):144. [Abstract]
- J Orthop Translat. 2022 Feb 17;32:112-120. [Abstract]
- Neural Regen Res. 2025 Mar 1;20(3):858-872. [Abstract]
- Mol Med. 2024 Apr 9;30(1):47. [Abstract]
- Br J Cancer. 2023 Feb;128(4):678-690. [Abstract]
- Cell Rep. 2019 Aug 27;28(9):2331-2344.e8. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- Cancer Cell Int. 2021 Jul 3;21(1):337. [Abstract]
- Front Immunol. 2021 Jan 21:11:610523. [Abstract]
- Eur J Med Chem. 2025 Nov 5:297:117918. [Abstract]
- Biochem Pharmacol. 2026 May:247:117810. [Abstract]
- Inflamm Res. 2023 Jul;72(7):1501-1512. [Abstract]
- J Cell Biol. 2025 Dec 1;224(12):e202502206. [Abstract]
- Commun Biol. 2020 Mar 17;3(1):128. [Abstract]
- Inflammation. 2021 Aug;44(4):1529-1539. [Abstract]
- Brain Pathol. 2020 Mar;30(2):373-385. [Abstract]
- Sci Rep. 2023 Jun 20;13(1):10041. [Abstract]
- Cancers (Basel). 2022 May 12;14(10):2377. [Abstract]
- J Magn Reson Imaging. 2025 Apr;61(4):1996-2008. [Abstract]
- J Biol Chem. 2024 Sep;300(9):107616. [Abstract]
- Hematol Oncol. 2024 Jan;42(1):e3233. [Abstract]
- Cancer Res Commun. 2023 Dec 27;3(12):2608-2622. [Abstract]
- Cancer Res Commun. 2022 Sep;2(9):1061-1074. [Abstract]
- J Immunol. 2021 Sep 1;207(5):1419-1427. [Abstract]
- Exp Cell Res. 2022 Nov 15;420(2):113361. [Abstract]
- Thromb Res. 2023 Aug:228:105-116. [Abstract]
- J Immunol Res. 2020 Jun 19:2020:4598476. [Abstract]
- Open Biol. 2017 May;7(5):170066. [Abstract]
- Phytochem Anal. 2026 Jan 20. [Abstract]
- Microvasc Res. 2022 Sep:143:104397. [Abstract]
- FEBS Open Bio. 2020 Dec;10(12):2578-2587. [Abstract]
- Biochem Biophys Res Commun. 2025 Aug 30:776:152209. [Abstract]
- Biochem Biophys Res Commun. 2024 May 21:709:149812. [Abstract]
- Biochem Biophys Res Commun. 2023 Oct 8:676:121-131. [Abstract]
- Exp Ther Med. 2022 Apr;23(4):302. [Abstract]
- J Histochem Cytochem. 2025 Jan-Feb;73(1-2):63-79. [Abstract]
- Res Sq. 2026 Feb 17.
- bioRxiv. 2025 Oct 26:2025.10.24.684367. [Abstract]
- bioRxiv. 2025 Aug 2:2025.07.31.667978. [Abstract]
- bioRxiv. 2024 November 06.
- bioRxiv. 2024 Feb 5.
- Patent. US20220380385A1.
- Research Square Preprint. 2021 Apr.
- Research Square Preprint. 2021 Mar.
- Ann Transl Med. 2020 Dec;8(23):1570. [Abstract]
- Patent. US20200330595A1.
- SSRN. 2020 May.
- bioRxiv. 2019 Sep.
- Patent. US20190231805A1.
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Histological Imaging/Staining
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Biological Activity
IC50: 70 nM (SHP2)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2200214-93-1
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Appearance Solid
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Molecular Weight 388.72
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Formula C16H20Cl3N5
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SMILES
NC1=NC(N2CCC(C)(N)CC2)=CN=C1C3=CC=CC(Cl)=C3Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (76)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Elaiophylin triggers paraptosis and preferentially kills ovarian cancer drug-resistant cells by inducing MAPK hyperactivation. [Abstract]2022 Sep 12;7(1):317. PMID: 36097006
SHP099 monohydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2022 Sep 12;7(1):317. [Abstract]
Assessment of indicated protein levels using western blotting in SKOV3 cells exposed to 0.5 µM elaiophylin for 24 h alone, or in combination with CHX (5 µM pretreatment for 4 h), U0126 (15 µM), SHP099 (30 µM), BAY293 (5 µM), respectively.
SHP099 monohydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2022 Sep 12;7(1):317. [Abstract]
SKOV3 cells were exposed to 0.5 µM elaiophylin alone for 36 h, or in combination with CHX (5 µM pretreatment for 4 h), U0126 (15 µM), SHP099 (30 µM), BAY293 (5 µM), respectively, and subject to enzymatic activity determination of CTSB.
SHP099 monohydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2022 Sep 12;7(1):317. [Abstract]
SHP099 (30 mg/kg/d). Representative images of tumor specimens stained with the specified antibody using immunohistochemical staining.
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Cancer Discov
SHP2 Inhibition Prevents Adaptive Resistance to MEK Inhibitors in Multiple Cancer Models. [Abstract]2018 Oct;8(10):1237-1249. PMID: 30045908
SHP099 monohydrochloride 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.
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Nat Immunol
Epithelial cells remove precancerous cells by cell competition via MHC class I-LILRB3 interaction. [Abstract]2021 Nov;22(11):1391-1402. PMID: 34686865 -
Cancer Res
SHP2-Mediated Inhibition of DNA Repair Contributes to cGAS-STING Activation and Chemotherapeutic Sensitivity in Colon Cancer. [Abstract]2021 Jun 15;81(12):3215-3228. PMID: 33820798 -
Cancer Res
NRAS Status Determines Sensitivity to SHP2 Inhibitor Combination Therapies Targeting the RAS-MAPK Pathway in Neuroblastoma. [Abstract]2020 Aug 15;80(16):3413-3423. PMID: 32586982 -
Nat Commun
2023 Apr 6;14(1):1933. PMID: 37024492 -
Nat Commun
Mitotic regulators and the SHP2-MAPK pathway promote IR endocytosis and feedback regulation of insulin signaling. [Abstract]2019 Apr 1;10(1):1473. PMID: 30931927
SHP099 monohydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 1;10(1):1473. [Abstract]
SHP099(10 μM; 24 h) inhibits IRS1-AP2 interaction in primary hepatocytes.
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Nat Commun
Mechanism of activating mutations and allosteric drug inhibition of the phosphatase SHP2. [Abstract]2018 Oct 30;9(1):4507. PMID: 30375376 -
Hepatology
Overriding Adaptive Resistance to Sorafenib Through Combination Therapy With Src Homology 2 Domain-Containing Phosphatase 2 Blockade in Hepatocellular Carcinoma. [Abstract]2020 Jul;72(1):155-168. PMID: 31610028 -
Hepatology
Hepatic stellate cell-derived platelet-derived growth factor receptor-alpha-enriched extracellular vesicles promote liver fibrosis in mice through SHP2. [Abstract]2018 Jul;68(1):333-348. PMID: 29360139
SHP099 monohydrochloride 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).
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Exp Mol Med
2020 Jun;52(6):911-920. PMID: 32576931 -
ACS Nano
Chimeric Peptide Engineered Bioregulator for Metastatic Tumor Immunotherapy through Macrophage Polarization and Phagocytosis Restoration. [Abstract]2023 Aug 22;17(16):16056-16068. PMID: 37578051 -
Mol Cell
HSPA1A and DNAJB1 regulate NELF condensate dynamics to safeguard transcriptional recovery under heat stress. [Abstract]2026 Feb 19;86(4):674-692.e10. PMID: 41653920 -
Mol Cell
A proteomic and phosphoproteomic landscape of KRAS mutant cancers identifies combination therapies. [Abstract]2021 Oct 7;81(19):4076-4090.e8. PMID: 34375582 -
Nat Chem Biol
2025 Aug;21(8):1226-1237. PMID: 39870764 -
Sci Transl Med
The inhibitory receptor Siglec-E controls antigen-presenting cell activation and T cell-mediated transplant rejection. [Abstract]2025 May 7;17(797):eads2694. PMID: 40333992 -
Theranostics
Targeting of glioma stem-like cells with a parthenolide derivative ACT001 through inhibition of AEBP1/PI3K/AKT signaling. [Abstract]2021 Jan 1;11(2):555-566. PMID: 33391492 -
Acta Pharm Sin B
Allosterically activating SHP2 by oleanolic acid inhibits STAT3-Th17 axis for ameliorating colitis. [Abstract]2024 Jun;14(6):2598-2612. PMID: 38828149 -
Acta Pharm Sin B
2022 Jul;12(7):3073-3084. PMID: 35865095 -
Acta Pharm Sin B
Allosteric inhibition reveals SHP2-mediated tumor immunosuppression in colon cancer by single-cell transcriptomics. [Abstract]2022 Jan;12(1):149-166. PMID: 35127377 -
J Clin Invest
THEMIS attenuates MASH by suppressing disease-associated hepatocyte induction and hepatocyte senescence in mice. [Abstract]2026 May 1;136(9):e199303. PMID: 42065240 -
MedComm (2020)
Tyrosine phosphatase SHP2 exacerbates psoriasis-like skin inflammation in mice via ERK5-dependent NETosis. [Abstract]2022 Mar 4;3(1):e120. PMID: 35281792 -
Neuro Oncol
2025 Mar 6:noaf057. PMID: 40045561 -
Neuro Oncol
Targeting PDGFRα-activated glioblastoma through specific inhibition of SHP-2-mediated signaling. [Abstract]2019 Nov 4;21(11):1423-1435. PMID: 31232447 -
J Control Release
Synergistic blockade of SHP-2 and A2AR signal pathways with targeted nanoparticles restores anti-tumor immunity of CD8+ T cells. [Abstract]2025 Aug 10:384:113889. PMID: 40425093 -
J Exp Med
Ferrous iron-activatable drug conjugate achieves potent MAPK blockade in KRAS-driven tumors. [Abstract]2022 Apr 4;219(4):e20210739. PMID: 35262628 -
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NPJ Precis Oncol
2024 Jul 16;8(1):144. PMID: 39014007 -
J Orthop Translat
Intraarticular injection of SHP2 inhibitor SHP099 promotes the repair of rabbit full-thickness cartilage defect. [Abstract]2022 Feb 17;32:112-120. PMID: 35228993 -
Neural Regen Res
Inhibiting SHP2 reduces glycolysis, promotes microglial M1 polarization, and alleviates secondary inflammation following spinal cord injury in a mouse model. [Abstract]2025 Mar 1;20(3):858-872. PMID: 38886958 -
Mol Med
Assessment of the FRET-based Teen sensor to monitor ERK activation changes preceding morphological defects in a RASopathy zebrafish model and phenotypic rescue by MEK inhibitor. [Abstract]2024 Apr 9;30(1):47. PMID: 38594640 -
Br J Cancer
Drug response profiles in patient-derived cancer cells across histological subtypes of ovarian cancer: real-time therapy tailoring for a patient with low-grade serous carcinoma. [Abstract]2023 Feb;128(4):678-690. PMID: 36476658 -
Cell Rep
Small-Molecule and CRISPR Screening Converge to Reveal Receptor Tyrosine Kinase Dependencies in Pediatric Rhabdoid Tumors. [Abstract]2019 Aug 27;28(9):2331-2344.e8. PMID: 31461650 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355 -
Cancer Cell Int
SHP2 inhibition enhances the anticancer effect of Osimertinib in EGFR T790M mutant lung adenocarcinoma by blocking CXCL8 loop mediated stemness. [Abstract]2021 Jul 3;21(1):337. PMID: 34217295 -
Front Immunol
SIRPα Suppresses Response to Therapeutic Antibodies by Nurse Like Cells From Chronic Lymphocytic Leukemia Patients. [Abstract]2021 Jan 21:11:610523. PMID: 33552071 -
Eur J Med Chem
2025 Nov 5:297:117918. PMID: 40609222 -
Biochem Pharmacol
An allosteric SHP2 inhibitor suppresses breast cancer-induced osteoclastogenesis and bone lysis. [Abstract]2026 May:247:117810. PMID: 41692348 -
Inflamm Res
2023 Jul;72(7):1501-1512. PMID: 37351631 -
J Cell Biol
2025 Dec 1;224(12):e202502206. PMID: 41100219 -
Commun Biol
Interaction of SHP-2 SH2 domains with PD-1 ITSM induces PD-1 dimerization and SHP-2 activation. [Abstract]2020 Mar 17;3(1):128. PMID: 32184441 -
Inflammation
2021 Aug;44(4):1529-1539. PMID: 33624224 -
Brain Pathol
Upregulated SHP-2 expression in the epileptogenic zone of temporal lobe epilepsy and various effects of SHP099 treatment on a pilocarpine model. [Abstract]2020 Mar;30(2):373-385. PMID: 31398269 -
Sci Rep
Mechanisms of synergistic suppression of ALK-positive lung cancer cell growth by the combination of ALK and SHP2 inhibitors. [Abstract]2023 Jun 20;13(1):10041. PMID: 37339995 -
Cancers (Basel)
Mutation of PTPN11 (Encoding SHP-2) Promotes MEK Activation and Malignant Progression in Neurofibromin-Deficient Cells in a Manner Sensitive to BRAP Mutation. [Abstract]2022 May 12;14(10):2377. PMID: 35625983 -
J Magn Reson Imaging
19Fluorine-MRI Based Longitudinal Immuno-Microenvironment-Monitoring for Pancreatic Cancer. [Abstract]2025 Apr;61(4):1996-2008. PMID: 39189434 -
J Biol Chem
2024 Sep;300(9):107616. PMID: 39089586 -
Hematol Oncol
Dependence of peripheral T-cell lymphoma on constitutively activated JAK3: Implication for JAK3 inhibition as a therapeutic approach. [Abstract]2024 Jan;42(1):e3233. PMID: 37876297 -
Cancer Res Commun
SHP2 inhibition with TNO155 increases efficacy and overcomes resistance of ALK inhibitors in neuroblastoma. [Abstract]2023 Dec 27;3(12):2608-2622. PMID: 38032104 -
Cancer Res Commun
Pharmacologic Inhibition of SHP2 Blocks Both PI3K and MEK Signaling in Low-epiregulin HNSCC via GAB1. [Abstract]2022 Sep;2(9):1061-1074. PMID: 36506869 -
J Immunol
Non-Lyn Src Family Kinases Activate SIRPα-SHP-1 to Inhibit PI3K-Akt2 and Dampen Proinflammatory Macrophage Polarization. [Abstract]2021 Sep 1;207(5):1419-1427. PMID: 34348974 -
Exp Cell Res
2022 Nov 15;420(2):113361. PMID: 36152731 -
Thromb Res
Role of SHP2 (PTPN11) in glycoprotein VI-dependent thrombus formation: Improved platelet responsiveness by the allosteric drug SHP099 in Noonan syndrome patients. [Abstract]2023 Aug:228:105-116. PMID: 37302266 -
J Immunol Res
Hypoxia Impairs NK Cell Cytotoxicity through SHP-1-Mediated Attenuation of STAT3 and ERK Signaling Pathways. [Abstract]2020 Jun 19:2020:4598476. PMID: 33123602 -
Open Biol
Targeting endogenous proteins for degradation through the affinity-directed protein missile system. [Abstract]2017 May;7(5):170066. PMID: 28490657
SHP099 monohydrochloride purchased from MedChemExpress. Usage Cited in: Open Biol. 2017 May;7(5):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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Phytochem Anal
2026 Jan 20. PMID: 41559525 -
Microvasc Res
Combination mTOR and SHP2 inhibitor treatment of lymphatic malformation endothelial cells. [Abstract]2022 Sep:143:104397. PMID: 35671835 -
FEBS Open Bio
SHP2 knockdown ameliorates liver insulin resistance by activating IRS-2 phosphorylation through the AKT and ERK1/2 signaling pathways. [Abstract]2020 Dec;10(12):2578-2587. PMID: 33012117 -
Biochem Biophys Res Commun
Shp2 regulates the trophoblast cell cycle progression through p53-p21 pathway modulation. [Abstract]2025 Aug 30:776:152209. PMID: 40527180 -
Biochem Biophys Res Commun
Allosteric SHP2 inhibition enhances regorafenib's effectiveness in colorectal cancer treatment. [Abstract]2024 May 21:709:149812. PMID: 38564942 -
Biochem Biophys Res Commun
Neonatal malnutrition impacts fibroblast growth factor 21-induced neuron neurite outgrowth and growth hormone-releasing hormone secretion in neonatal mouse brain. [Abstract]2023 Oct 8:676:121-131. PMID: 37506473 -
Exp Ther Med
Shp2 suppresses fat accumulation in white adipose tissue by activating Wnt/β-catenin signaling following vertical sleeve gastrectomy in obese rats with type-2 diabetes. [Abstract]2022 Apr;23(4):302. PMID: 35340882 -
J Histochem Cytochem
Development of an ALK-positive Non-Small-Cell Lung Cancer in Vitro Tumor 3D Culture Model for Therapeutic Screening. [Abstract]2025 Jan-Feb;73(1-2):63-79. PMID: 39991927 -
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bioRxiv
Synergistic effects of deleting the tyrosine phosphatases Shp1 and Shp2 on megakaryopoiesis and thrombopoiesis in mice. [Abstract]2025 Oct 26:2025.10.24.684367. PMID: 41279089 -
bioRxiv
2025 Aug 2:2025.07.31.667978. PMID: 40766426 -
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Ann Transl Med
Uric acid preconditioning alleviated doxorubicin induced JNK activation and Cx43 phosphorylation associated cardiotoxicity via activation of AMPK-SHP2 signaling pathway. [Abstract]2020 Dec;8(23):1570. PMID: 33437769 -
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Solvent & Solubility
DMSO : 4.1 mg/mL (10.55 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 2.5 mg/mL (6.43 mM)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.43 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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 20 mg/mL (51.45 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82. [Content Brief]
[2]. 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]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.5725 mL | 12.8627 mL | 25.7255 mL | 64.3136 mL |
| 5 mM | 0.5145 mL | 2.5725 mL | 5.1451 mL | 12.8627 mL | |
| DMSO | 10 mM | 0.2573 mL | 1.2863 mL | 2.5725 mL | 6.4314 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.