TargetMol

SHP099

Product Code:
 
TAR-T3564
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T3564-1mg1mg£95.00
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TAR-T3564-2mg2mg£106.00
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TAR-T3564-1mL1 mL * 10 mM (in DMSO)£115.00
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TAR-T3564-5mg5mg£128.00
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TAR-T3564-10mg10mg£152.00
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TAR-T3564-25mg25mg£213.00
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TAR-T3564-50mg50mg£261.00
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TAR-T3564-100mg100mg£417.00
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Further Information

Bioactivity:
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.
CAS:
1801747-42-1
Formula:
C16H19Cl2N5
Molecular Weight:
352.26
Pathway:
Apoptosis; Metabolism
Purity:
0.9873
SMILES:
CC1(N)CCN(CC1)c1cnc(c(N)n1)-c1cccc(Cl)c1Cl
Target:
Phosphatase; PERK

References

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. 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. 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. P?dua 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. Yang N, Fan Z, Sun S, et al.Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation.European Journal of Medicinal Chemistry.2023: 115857.