2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. SHP2 Phosphatase
  4. Batoprotafib

Batoprotafib  (Synonyms: TNO155)

Cat. No.: HY-136173 Purity: 99.41%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Batoprotafib Chemical Structure

Batoprotafib Chemical Structure

CAS No. : 1801765-04-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
1 mg USD 133 In-stock
5 mg USD 280 In-stock
10 mg USD 390 In-stock
25 mg USD 780 In-stock
50 mg USD 1150 In-stock
100 mg USD 1950 In-stock
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Based on 5 publication(s) in Google Scholar

Batoprotafib Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].
IC50 & Target

IC50: 0.011 µM (SHP2)[1]
In Vitro

Batoprotafib 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[1].
Batoprotafib (0-1000 nM; 6 days) inhibits the viability of NCI-H3255, HCC827, and PC9 cells with IC50 values lower than 1.5 μM. Batoprotafib is efficacious in EGFR-mutant NSCLC cell lines[2].
Batoprotafib is efficacious in acquired resistance models of EGFR inhibitors and demonstrates combination benefit with EGFR inhibitors[2].
Batoprotafib enhances the efficacy of KRASG12C inhibitors against KRASG12C lung and colorectal cancers[2].
Batoprotafib inhibits immune-suppressive macrophages and synergizes with PD1 blockade[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Batoprotafib Related Antibodies

Cell Proliferation Assay[2]

Cell Line: PC-9, PC-9 EGFRT790M/C797S, HCC827, HCC827-GR (gefinitib-resistant)
Concentration: 0-1000 nM
Incubation Time: 6 days
Result: Inhibited cell viability with IC50s of 1.56, 1.38, 0.77 and 1.38 μM against PC-9 and PC-9 EGFRT790M/C797S, HCC827 and HCC827-GR cells, respectively.

Western Blot Analysis[2]

Cell Line: PC-14 (EGFRex19del)
Concentration: 3 μM
Incubation Time: 4h and 24 h
Result: Effectively reduced p-ERK levels at 4 hours but suffered a rebound at 24 hours.
In Vivo

The oral bioavailability in mouse, rat and money are 78%, 86%, and 60%, respectively[1].
Batoprotafib (20 mg/kg; p.o.; twice daily for 40 days) inhibits tumor growth and is more effective when combined with Dabrafenib (HY-14660) plus Trametinib (HY-10999) in nude mice bearing HT-29 xenografts[2].
Batoprotafib (7.5 mg/kg; p.o.; b.i.d. or q.d. for 36 days) plus JDQ-443 (HY-139612) (100 mg/kg; p.o.; q.d.) improves the single-agent activity of JDQ443 in KRASG12C-mutated cell-derived (CDX) models in nude mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice bearing HT-29 xenografts[2]
Dosage: 20 mg/kg alone or 10 mg/kg in combination with Dabrafenib and Trametinib
Administration: PO, twice daily for 40 days
Result: Resulted in moderate tumor growth inhibition. Maintained tumor stasis for more than 40 days when combined with Dabrafenib plus Trametinib.
Clinical Trial
Molecular Weight

421.95

Formula

C18H24ClN7OS
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

N[C@@H]1[C@H](C)OCC12CCN(C3=NC(N)=C(SC4=C(Cl)C(N)=NC=C4)N=C3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (236.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.41%

COA (248 KB) HNMR (400 KB) RP-HPLC (206 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3699 mL 11.8497 mL 23.6995 mL 59.2487 mL
5 mM 0.4740 mL 2.3699 mL 4.7399 mL 11.8497 mL
10 mM 0.2370 mL 1.1850 mL 2.3699 mL 5.9249 mL
15 mM 0.1580 mL 0.7900 mL 1.5800 mL 3.9499 mL
20 mM 0.1185 mL 0.5925 mL 1.1850 mL 2.9624 mL
25 mM 0.0948 mL 0.4740 mL 0.9480 mL 2.3699 mL
30 mM 0.0790 mL 0.3950 mL 0.7900 mL 1.9750 mL
40 mM 0.0592 mL 0.2962 mL 0.5925 mL 1.4812 mL
50 mM 0.0474 mL 0.2370 mL 0.4740 mL 1.1850 mL
60 mM 0.0395 mL 0.1975 mL 0.3950 mL 0.9875 mL
80 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7406 mL
100 mM 0.0237 mL 0.1185 mL 0.2370 mL 0.5925 mL
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Batoprotafib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Batoprotafib1801765-04-7TNO155TNO 155TNO-155SHP2PhosphataseSrc homology phosphatase 2PTPN11RTK-dependentmalignancyAberrantactivationBCSallostericEGFR-mutantNSCLCHNSCCCRCInhibitorinhibitorinhibit

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