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SHP2 Phosphatase Inhibitor
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SHP099
SHP099
SHP099 is a highly potent (IC50 = 71 nM), selective and orally bioavailable small-molecule SHP2 inhibitor that stabilizes SHP2 in an auto-inhibited conformation. It 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 signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro and is efficacious in mouse tumour xenograft models (ref. 1). Inhibition of SHP2 by SHP099 also triggers anti-tumor immunity and synergizes with PD-1 blockade (ref. 2).
Catalog NO:
CT-SHP099
Synonym:
SHP-099
CAS NO:
1801747-11-4 (HCl salt) 1801747-42-1 (free base)
Mol. Formula:
C16H19Cl2N5 ∙ 2HCl
MW:
425.1
** 99.9% Pure, in vivo Quality Material. A yellow powder, with multi cycle recrystallizations. Dihydrochloride, validated by a spot-on Quantitative Elemental Analysis. Made for in vivo studies. Bulk Stock!! Same Day Shipping.
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10 mg
$80.00
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Solubility :
Refer to Certificate
Storage :
Refer to Certificate
Purity :
99.9% by HPLC at 214 and 254 nm
Original QC Data :
HPLC, NMR, and Quantitative Elemental Analysis Report
Please Pick Batch NO:
6
CHEMIETEK, SHP099, Lot 06, LC-MS.pdf
CHEMIETEK, SHP099, Lot 06, NMR.pdf
SHP099, Lot 06, Certificate of Analysis.pdf
1: YP Chen, et al, Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature, 2016 Jun 29;535(7610):148-152. doi: 10.1038/nature18621.
2. Zhao, M. X, et al. SHP2 inhibition triggers anti-tumor immunity and synergizes with PD-1 blockade. Acta Pharmaceutica Sinica B (2018), https://doi.org/10.1016/j.apsb.2018.08.009
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