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SHP099

Catalog No. T3564 CAS 1801747-42-1

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

SHP099 free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.

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SHP099, CAS 1801747-42-1

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SHP099 free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.
Targets&IC50	p-ERK:0.250 μM, SHP2:0.07 μM

Synonyms	SHP099 free base, SHP 099, SHP-099
Molecular Weight	352.26
Formula	C16H19Cl2N5
CAS No.	1801747-42-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 5.5 mg/mL (15.61 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. LaRochelle JR, Fodor M, Vemulapalli V, Mohseni M, Wang P, Stams T, LaMarche MJ, Chopra R, Acker MG, Blacklow SC. Structural reorganization of SHP2 by oncogenic mutations and implications for oncoprotein resistance to allosteric inhibition. Nat Commun. 2018 Oct 30;9(1):4508. doi: 10.1038/s41467-018-06823-9. 2. Pádua RAP, Sun Y, Marko I, Pitsawong W, Stiller JB, Otten R, Kern D. Mechanism of activating mutations and allosteric drug inhibition of the phosphatase SHPNat Commun. 2018 Oct 30;9(1):4507. doi: 10.1038/s41467-018-06814-w. PubMed PMID: 30375376; PubMed Central PMCID: PMC6207724. 3. Hill KS, Roberts ER, Wang X, Marin E, Park TD, Son S, Ren Y, Fang B, Yoder S, Kim S, Wan L, Sarnaik AA, Koomen JM, Messina JL, Teer JK, Kim Y, Wu J, Chalfant CE, Kim M. PTPN11 plays oncogenic roles and is a therapeutic target for BRAF wild-type melanomas. Mol Cancer Res. 2018 Oct 2pii: molcanres.0777.2018. doi: 10.1158/1541-7786.MCR-18-0777. [Epub ahead of print] PubMed PMID: 30355677. 4. Fedele C, Ran H, Diskin B, Wei W, Jen J, Geer MJ, Araki K, Ozerdem U, Simeone DM, Miller G, Neel BG, Tang KH. SHP2 Inhibition Prevents Adaptive Resistance to MEK Inhibitors in Multiple Cancer Models. Cancer Discov. 2018 Oct;8(10):1237-1249. doi: 10.1158/2159-8290.CD-18-044Epub 2018 Jul 2PubMed PMID: 30045908; PubMed Central PMCID: PMC6170706.

Related Products

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Rocaglamide 2BAct BTdCPU ISRIB (trans-isomer) SHP099 Briciclib 4EGI-1 GSK2606414

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SHP099 1801747-42-1 代谢凋亡 PERK Phosphatase SHP099 free base inhibit SHP-099 SHP 099 Inhibitor inhibitor

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