SHP099 xHCl --- SHP2 Phosphatase Inhibitor


Catalog No. size PriceQuantity
M60319-2S 2 mg solid $139
M60319-10S 10mg solid $556

Description

SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM. SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest.

Product information

CAS Number: 1801747-11-4

Molecular Weight: 352.26

Formula: C16H19Cl2N5

Chemical Name: 6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine hydrochloride

Smiles: CC1(N)CCN(CC1)C1=CN=C(C2=CC=CC(Cl)=C2Cl)C(N)=N1

InChiKey: YGUFCDOEKKVKJK-UHFFFAOYSA-N

InChi: InChI=1S/C16H19Cl2N5/c1-16(20)5-7-23(8-6-16)12-9-21-14(15(19)22-12)10-3-2-4-11(17)13(10)18/h2-4,9H,5-8,20H2,1H3,(H2,19,22)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

SHP099 was used at 10 µM in vitro and cellular assays.

In Vivo:

SHP099 was dosed orally to mouse tumor xenograft models at 75-100 mg/Kg once per day.

References:

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

Products are for research use only. Not for human use.


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