Batoprotafib
Based on 7 publication(s) in Google Scholar
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.
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- 純度: 99.89%
- CAS 番号: 1801765-04-7
- 分子式: C18H24ClN7OS
- 分子量:421.95
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Batoprotafib
More- Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8. [Abstract]
- Nat Commun. 2023 Apr 6;14(1):1933. [Abstract]
- Eur J Cancer. 2021 Dec:159:16-23. [Abstract]
- J Med Chem. 2026 Feb 26;69(4):3932-3940.
- Cancer Res Commun. 2023 Dec 27;3(12):2608-2622. [Abstract]
- Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
- bioRxiv. 2026 Jun 25.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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RT-PCR
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WB
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Cell Proliferation/Viability Assay
生物活性
IC50: 0.011 µM (SHP2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EMT6 | IC50 |
2.49 μM
Compound: TNO155
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Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of abemaciclib by MTT assay
Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of abemaciclib by MTT assay
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[PMID: 35447031] |
| EMT6 | IC50 |
7.03 μM
Compound: TNO155
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Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 35447031] |
| KYSE-520 cell line | IC50 |
0.1 μM
Compound: 1, TNO155
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Antiproliferative activity against human KYSE-520 cells
Antiproliferative activity against human KYSE-520 cells
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[PMID: 32910655] |
| MDA-MB-231 | IC50 |
>20 μM
Compound: TNO155
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 35447031] |
| MDA-MB-231 | IC50 |
12.94 μM
Compound: TNO155
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of abemaciclib by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of abemaciclib by MTT assay
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[PMID: 35447031] |
| MDA-MB-468 | IC50 |
>20 μM
Compound: TNO155
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 35447031] |
| MDA-MB-468 | IC50 |
3.11 μM
Compound: TNO155
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of abemaciclib by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of abemaciclib by MTT assay
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[PMID: 35447031] |
| MV4-11 | IC50 |
39 nM
Compound: 8; TNO155
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
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[PMID: 39303516] |
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.
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Cell Line:PC-9, PC-9 EGFRT790M/C797S, HCC827, HCC827-GR (gefinitib-resistant)
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Concentration:0-1000 nM
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Incubation Time:6 days
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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.
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Cell Line:PC-14 (EGFRex19del)
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Concentration:3 μM
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Incubation Time:4h and 24 h
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Result:Effectively reduced p-ERK levels at 4 hours but suffered a rebound at 24 hours.
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.
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Animal Model:Female athymic nude mice bearing HT-29 xenografts[2]
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Dosage:20 mg/kg alone or 10 mg/kg in combination with Dabrafenib and Trametinib
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Administration:PO, twice daily for 40 days
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Result:Resulted in moderate tumor growth inhibition. Maintained tumor stasis for more than 40 days when combined with Dabrafenib plus Trametinib.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1801765-04-7
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性状 Solid
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分子量 421.95
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分子式 C18H24ClN7OS
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Color Off-white to yellow
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SMILES
N[C@@H]1[C@H](C)OCC12CCN(C3=NC(N)=C(SC4=C(Cl)C(N)=NC=C4)N=C3)CC2
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別名
TNO155
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026
Batoprotafib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8. [Abstract]
Dose-response curves of inhibitor targeting SHP2 (Batoprotafib (0.1-500 nM)) (top left). Dose-response curves of HRS-4642 (bottom left), and growth inhibition matrices of indicated inhibitor combined with HRS-4642 (right) in FC1242.
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Nat Commun
2023 Apr 6;14(1):1933. PMID: 37024492
Batoprotafib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Apr 6;14(1):1933. [Abstract]
Tumor proliferation in mice engrafted with chordoma cells (U-CH1 cell line-derived xenograft, CF539 PDX, or CF466 PDX) and treated with a SHP2 inhibitor (RMC-4550 or Batoprotafib (TNO155) (20 mg/kg; p.o.)). Points represent the mean tumor volume ± s.e.m. (n = 4 (control) or 5 (compound) tumors for each arm of the U-CH1/RMC-4550 study; n = 6 (compound) or 7 (control) tumors for each arm of the U-CH1/TNO155 study; n = 6 (control) or 7 (compound) tumors for each arm of the CF539 study; n = 7 tumors for each arm of the CF466 study).
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Eur J Cancer
HER2 mediates clinical resistance to the KRASG12C inhibitor sotorasib, which is overcome by co-targeting SHP2. [Abstract]2021 Dec:159:16-23. PMID: 34715459 -
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Cancer Res Commun
SHP2 inhibition with TNO155 increases efficacy and overcomes resistance of ALK inhibitors in neuroblastoma. [Abstract]2023 Dec 27;3(12):2608-2622. PMID: 38032104
Batoprotafib purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2023 Dec 27;3(12):2608-2622. [Abstract]
Calculation of IC50 in neuroblastoma cells following treatment with Batoprotafib (TNO155) for 72 hours. **, P < 0.01; ***, P < 0.001.
Batoprotafib purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2023 Dec 27;3(12):2608-2622. [Abstract]
Western immunoblots of Kelly and SH-SY5Y cells treated with Batoprotafib (TNO155) (1 µmol/L), lorlatinib (1 µmol/L), or combination for 24 hours. Batoprotafib (TNO155) plus lorlatinib treatment showed marked inhibition of ALK and SHP2 activity, including inactivation of MAPK downstream signaling.
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Int J Biochem Cell Biol
MEST promotes immune escape in gastric cancer by downregulating MHCI expression via SHP2. [Abstract]2024 Sep:174:106621. PMID: 39181599
Batoprotafib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
Co-culture of three different groups of GC cells (oe-NC+DMSO, oe-NC+TNO155 (Batoprotafib) (1 μM; 24 h), oe-MEST+TNO155) with CD8+ T cells; qPCR detection of the expression of MHCI-related genes and SHP2 in GC cells. The results showed that TNO155 significantly promoted the expression of MCHI-related genes, and oe-MEST+TNO155 partially reversed the increase in MCHI-related gene expression.
Batoprotafib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
Co-culture of three different groups of GC cells (oe-NC+DMSO, oe-NC+TNO155 (Batoprotafib) (1 μM; 24 h), oe-MEST+TNO155) with CD8+ T cells; WB detection of the expression of MHCI-related genes and SHP2 in GC cells. The results showed that TNO155 significantly inhibited SHP2 expression, and oe-MEST+TNO155 restored SHP2 expression to the control group level.
Batoprotafib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
LDH assay of cytotoxicity of CD8+ T cells. The results showed that TNO155 (Batoprotafib) (1 μM; 24 h) significantly enhanced the killing of HGC-27 cells by CD8+ T cells, and further overexpression of MEST attenuated the increased cytotoxicity of CD8+ T cells.
Batoprotafib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
Flow cytometry analysis of cellular apoptosis. The results showed that compared to the control group, TNO155 (Batoprotafib) (1 μM; 24 h) significantly increased the apoptotic rate of HGC-27 cells, while further overexpression of MEST significantly reduced the apoptotic rate of HGC-27 cells.
Batoprotafib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
ELISA measurement of concentration of IFN-γ in cell culture supernatant. ELISA results indicated that compared to the control group, TNO155 (Batoprotafib) (1 μM; 24 h) significantly increased the levels of IFN-γ and TNF-α in the supernatant of HGC-27 cells, while after overexpression of MEST, the levels of IFN-γ and TNF-α in the supernatant were significantly reduced.
Batoprotafib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2024 Sep:174:106621. [Abstract]
Transwell measurement of the migration of GC cells after co-culturing with CD8+ T cells. Transwell assays revealed that the migration and invasion abilities of HGC-27 cells were significantly reduced upon the addition of TNO155 (Batoprotafib) (1 μM; 24 h), while in the oe-MEST+TNO155, the migration and invasion abilities of the tumor cells were restored to the control group level.
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溶剤 & 溶解度
DMSO : 66.67 mg/mL (158.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (280 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Liu C, et al. Combinations with Allosteric SHP2 Inhibitor TNO155 to Block Receptor Tyrosine Kinase Signaling. Clin Cancer Res. 2021 Jan 1;27(1):342-354. [Content Brief]
[3]. Weiss A, et al. Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C. Cancer Discov. 2022 Jun 2;12(6):1500-1517. [Content Brief]
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 |
Batoprotafib 関連分類
HY-136173 関連分類
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