| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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Purity: ≥98%
TNO155 (TNO-155) is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11; IC50=11 nM) with potential anticancer activity. Activating the RAS-RAF-ERK signaling pathway, SHP2 is an oncoprotein that is overexpressed in many types of cancer cells. It regulates cell survival, migration, and proliferation. Additionally, SHP2 controls immune checkpoint modulation and signal transduction mediated by programmed cell death 1 (PD-1). Researching RTK-dependent cancers, particularly advanced solid tumors, may benefit from the use of TNO155.
| Targets |
SHP2 (IC50 = 0.011 µM)
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|---|---|
| ln Vitro |
TNO155 has an IC50 of 0.008 µM for KYSE520 pERK and 0.100 µM for KYSE520 5-day cell proliferation, respectively. For Cav1.2, VMAT, SST3, and all other compounds, the corresponding off-target IC50 values are 18 µM, 6.9 µM, 11 µM, and > 30μM.[1]
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| ln Vivo |
TNO155 is a first-in-class, highly oral bioavailable, and BCS class I inhibitor of wild-type SHP2 that is both potent and selective. TNO155 has an oral bioavailability of 78%, 86%, and 60% in mice, rats, and money, respectively.[1]
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| Cell Assay |
PC-14 cells were subjected to 4 or 24 hours of treatment with nazartinib (0.1 or 0.3 µM), 3 µM TNO155, or the combination of nazartinib and TNO155.
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| References | |
| Additional Infomation |
Batoprotafib is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11), with potential antineoplastic activity. Upon oral administration,batoprotafib binds to and inhibits SHP2. This prevents SHP2-mediated signaling, inhibits MAPK signaling and prevents growth of SHP2-expressing tumor cells. SHP2, an oncoprotein overexpressed in a variety of cancer cell types, regulates cell survival, differentiation and proliferation through activation of the RAS-RAF-ERK signaling pathway. SHP2 also regulates programmed cell death 1 (PD-1)-mediated signal transduction and is involved in immune checkpoint modulation.
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| Molecular Formula |
C18H24CLN7OS
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|---|---|
| Molecular Weight |
421.9475
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| Exact Mass |
421.145
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| Elemental Analysis |
C, 51.24; H, 5.73; Cl, 8.40; N, 23.24; O, 3.79; S, 7.60
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| CAS # |
1801765-04-7
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| Related CAS # |
1801765-04-7
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| PubChem CID |
118238370
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| Appearance |
Off-white to yellow solid powder
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
538
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@H]1[C@H](C2(CCN(CC2)C3=CN=C(C(=N3)N)SC4=C(C(=NC=C4)N)Cl)CO1)N
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| InChi Key |
UCJZOKGUEJUNIO-IINYFYTJSA-N
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| InChi Code |
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
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| Chemical Name |
(3S,4S)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine
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| Synonyms |
batoprotafib; TNO-155; TNO155; TNO 155
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 84~100 mg/mL (199.1~237 mM)
Ethanol: ~5 mg/mL (11.9 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3699 mL | 11.8497 mL | 23.6995 mL | |
| 5 mM | 0.4740 mL | 2.3699 mL | 4.7399 mL | |
| 10 mM | 0.2370 mL | 1.1850 mL | 2.3699 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04000529 | Active Recruiting |
Drug: TNO155 Drug: Ribociclib |
Esophageal SCC Colorectal Cancer |
Novartis Pharmaceuticals | July 30, 2019 | Phase 1 |
| NCT04330664 | Active Recruiting |
Drug: TNO155 Drug: MRTX849 |
Advanced Cancer Metastatic Cancer |
Mirati Therapeutics Inc. | April 22, 2020 | Phase 1 Phase 2 |
| NCT05541159 | Not yet recruiting | Drug: TNO155 | Renal Impairment | Novartis Pharmaceuticals | February 15, 2024 | Phase 1 |
| NCT05490030 | Not yet recruiting | Drug: TNO155 | Hepatic Impairment | Novartis Pharmaceuticals | February 19, 2024 | Phase 1 |
| NCT04699188 | Recruiting | Drug: TNO155 Drug: JDQ443 |
Cancer of Lung Lung Cancer |
Novartis Pharmaceuticals | February 24, 2021 | Phase 1 Phase 2 |
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