TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.

Product information

CAS Number: 1801765-04-7

Molecular Weight: 421.95

Formula: C18H24ClN7OS

Chemical Name: (3S,4S)-8-{6-amino-5-[(2-amino-3-chloropyridin-4-yl)sulfanyl]pyrazin-2-yl}-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine

Smiles: C[C@@H]1OCC2(CCN(CC2)C2=CN=C(SC3=CC=NC(N)=C3Cl)C(N)=N2)[C@@H]1N

InChiKey: UCJZOKGUEJUNIO-IINYFYTJSA-N

InChi: InChI=1S/C18H24ClN7OS/c1-10-14(20)18(9-27-10)3-6-26(7-4-18)12-8-24-17(16(22)25-12)28-11-2-5-23-15(21)13(11)19/h2,5,8,10,14H,3-4,6-7,9,20H2,1H3,(H2,21,23)(H2,22,25)/t10-,14+/m0/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 100 mg/mL (236.99 mM; Need ultrasonic).

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:

TNO155 shows an IC50 of 0.008 µM in KYSE520 pERK assay and shows an IC50 of 0.100 µM in KYSE520 5-day cell proliferation assay. The off-target IC50 values are 18 µM, 6.9 µM, and 11 µM for Cav1.2, VMAT, and SST3, respectively.

In Vivo:

The oral bioavailability in mouse, rat and money are 78%, 86%, and 60%, respectively.

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