Batoprotafib(TNO155)

Batoprotafib(TNO155) is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2 /src homology region 2 domain phosphatase /PTPN11) with IC50 of 0.011 µM. TNO155 has potential antineoplastic activity.

Batoprotafib(TNO155) Chemical Structure

Batoprotafib(TNO155) Chemical Structure

CAS: 1801765-04-7

Selleck's Batoprotafib(TNO155) has been cited by 4 publications

Purity & Quality Control

Batch: S898701 DMSO] 84 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.44%
99.44

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Biological Activity

Description Batoprotafib(TNO155) is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2 /src homology region 2 domain phosphatase /PTPN11) with IC50 of 0.011 µM. TNO155 has potential antineoplastic activity.
Targets
SHP-2 [1]
(Cell-free assay)
0.011 μM
In vitro
In vitro

TNO155 inhibits KYSE520 pERK and KYSE520 5-day cell proliferation with IC50 of 0.008 µM and of 0.100 µM, respectively. The off-target IC50 are 18 µM, 6.9 µM, 11 µM and > 30μM for Cav1.2, VMAT, SST3 and all others, respectively.[1]

Cell Research Cell lines PC-14 cells
Concentrations 3 μM
Incubation Time 24 h
Method

PC-14 cells were treated with nazartinib (0.1 or 0.3 µM), 3 µM TNO155, or the combination of nazartinib and TNO155 for 4 hours or 24 hours.

In Vivo
In vivo

TNO155 is a potent and selective first-in-class inhibitor of wild-type SHP2, with high oral bioavailability and BCS class I properties. The oral bioavailability of TNO155 in mouse, rat and money are 78%, 86%, and 60%, respectively.[1]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05541159 Not yet recruiting
Renal Impairment
Novartis Pharmaceuticals|Pharmaceutical Research Associates|Novartis
February 15 2024 Phase 1
NCT05490030 Not yet recruiting
Hepatic Impairment
Novartis Pharmaceuticals|Pharmaceutical Research Associates|Novartis
February 19 2024 Phase 1
NCT04330664 Active not recruiting
Advanced Cancer|Metastatic Cancer|Malignant Neoplastic Disease
Mirati Therapeutics Inc.|Novartis
April 22 2020 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 421.95 Formula

C18H24ClN7OS

CAS No. 1801765-04-7 SDF --
Density g/mL
Smiles CC1C(C2(CCN(CC2)C3=CN=C(C(=N3)N)SC4=C(C(=NC=C4)N)Cl)CO1)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (199.07 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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