SNX-2112
Based on 4 publication(s) in Google Scholar
SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 908112-43-6
- Formula: C23H27F3N4O3
- Molecular Weight:464.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) SNX-2112
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Biological Activity
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HSP90α 30 nM (IC50) |
HSP90β 30 nM (IC50) |
GRP94 4275 nM (IC50) |
TRAP-1 862 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
1 nM
Compound: 9, SNX-2112
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Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening
Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening
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[PMID: 19552433] |
| A-375 | IC50 |
2 nM
Compound: 9, SNX-2112
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Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening
Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening
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[PMID: 19552433] |
| A-375 | IC50 |
23 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| AU565 | IC50 |
10 μM
Compound: 9, SNX-2112
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Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening
Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening
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[PMID: 19552433] |
| AU565 | IC50 |
41 nM
Compound: 9, SNX-2112
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Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening
Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening
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[PMID: 19552433] |
| HCT-15 | IC50 |
52 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| HT-29 | IC50 |
3 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| J774.A1 | IC50 |
<0.06 μM
Compound: SNX2112; 1
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Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
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[PMID: 28835791] |
| K562 | IC50 |
6 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| LNCaP | IC50 |
3 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| MCF7 | EC50 |
19 nM
Compound: 13b, PF-4928473, SNX-2112
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Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
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[PMID: 22938030] |
| MCF7 | IC50 |
22 nM
Compound: 9, SNX-2112
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Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
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[PMID: 20055425] |
| MCF7 | IC50 |
53 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| MDA-MB-231 | IC50 |
6 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| MRC5 | CC50 |
21.34 μM
Compound: SNX-2112
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Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
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[PMID: 22704890] |
| NCI-H460 | IC50 |
18 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| PC-3 | IC50 |
17 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| SK-MEL-5 | IC50 |
6 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| SW-620 | IC50 |
3 nM
Compound: 9, SNX-2112
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Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method
Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method
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[PMID: 19552433] |
| Vero | CC50 |
13.33 μM
Compound: SNX-2112
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Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay
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[PMID: 22704890] |
| Vero | EC50 |
1.85 μM
Compound: SNX-2112
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Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay
Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay
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[PMID: 22704890] |
| Vero | EC50 |
2.26 μM
Compound: SNX-2112
|
Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay
Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay
|
[PMID: 22704890] |
SNX-2112 is an orally active Hsp90 inhibitor, with a Kd of 16 nM, and also induces Her-2 degradation, with an IC50 of 10 nM[3]. SNX-2112 binds to Hsp90, with IC50s of 30 nM, 30 nM, 4.275 μM and 0.862 μM for Hsp90 α and β, Grp94 and Trap-1, respectively[1]. SNX-2112 shows potent antiproliferative activity against various cancer cell types, with IC50s of 3 nM to 53 nM. SNX-2112 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC50s of 11 ± 5, 41 ± 12, and 1 ± 0.6 nM, respectively. SNX-2112 also induces Hsp70 in A375 cells with an IC50 of 2 ± 0.9 nM[3]. In addition, SNX-2112 potently blocks signaling of Hsp90 clients, such as Akt, ERK, and NF-κB pathways in different cells. SNX-2112 inhibits multiple myeloma (MM) cell growth, including MM.1S, U266, INA-6, RPMI8226, OPM1, OPM2, MM.1R, and Dox40 MM cell lines, with IC50s of 52, 55, 19, 186, 89, 67, 93, and 53 nM at 48 hours, respectively. SNX-2112 (2.5-10 nM) also suppresses osteoclast formation, associated with down-regulation of ERK/c-fos and PU.1[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 908112-43-6
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Appearance Solid
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Molecular Weight 464.48
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Formula C23H27F3N4O3
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Color White to off-white
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SMILES
FC(F)(C1=NN(C2=CC(N[C@@H]3CC[C@H](CC3)O)=C(C=C2)C(N)=O)C(CC(C)(C4)C)=C1C4=O)F
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Synonyms
PF-04928473
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Theranostics
Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]2019 Aug 12;9(20):5769-5783. PMID: 31534518 -
Antioxidants (Basel)
A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]2026 May 12;15(5):612. PMID: 42193234 -
J Mater Chem B
Suppression of the HSP90-HIF1α pathway with SNX2112-encapsulated nano-micelles for effective triple-negative breast cancer photothermal combined photodynamic therapy. [Abstract]2025 Jul 2;13(26):7753-7768. PMID: 40468772 -
J Pharm Biomed Anal
Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method for quantification of SR1001, an inverse agonist of retinoid-related orphan receptors, and its application to pharmacokinetic studies in streptozotocin-induced diabetic mice. [Abstract]2017 Sep 5:143:94-100. PMID: 28578255
Solvent & Solubility
DMSO : 25 mg/mL (53.82 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.38 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 (5.38 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.
Protocol
To measure proliferation of multiple myeloma (MM) cells and bone marrow stromal cells (BMSCs), the rate of DNA synthesis is measured. MM cells are incubated in 96-well culture plates in the presence of SNX-2112 and/or IL-6 or IGF-1 or BMSCs for 48 hours. Cells are pulsed with 0.5 μCi/well of [3H]-thymidine during the last 8 hours of culture, harvested onto glass filters with an automatic cell harvester, and counted using the LKB Betaplate scintillation counter. Inhibition of proliferation by test compounds (SNX-2112) in solid tumor cell lines is measured in 96-well plates after 72 hours of treatment with Cyquant DNA binding dye. AML, LCL, and K562 cell line proliferation rates are measured after 72 hours of compound treatment with CellTiter-Glo[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Chandarlapaty S, et al. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res. 2008 Jan 1;14(1):240-8. [Content Brief]
[2]. Mishra SJ, et al. Transformation of the Non-Selective Aminocyclohexanol-Based Hsp90 Inhibitor into a Grp94-Seletive Scaffold. ACS Chem Biol. 2017 Jan 20;12(1):244-253. [Content Brief]
[3]. Huang KH, et al. Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. J Med Chem. 2009 Jul 23;52(14):4288-305 [Content Brief]
[4]. Okawa Y, et al. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood. 2009 Jan 22;113(4):846-55. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1529 mL | 10.7647 mL | 21.5295 mL | 53.8236 mL |
| 5 mM | 0.4306 mL | 2.1529 mL | 4.3059 mL | 10.7647 mL | |
| 10 mM | 0.2153 mL | 1.0765 mL | 2.1529 mL | 5.3824 mL | |
| 15 mM | 0.1435 mL | 0.7176 mL | 1.4353 mL | 3.5882 mL | |
| 20 mM | 0.1076 mL | 0.5382 mL | 1.0765 mL | 2.6912 mL | |
| 25 mM | 0.0861 mL | 0.4306 mL | 0.8612 mL | 2.1529 mL | |
| 30 mM | 0.0718 mL | 0.3588 mL | 0.7176 mL | 1.7941 mL | |
| 40 mM | 0.0538 mL | 0.2691 mL | 0.5382 mL | 1.3456 mL | |
| 50 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0765 mL |