WP1066
Based on 39 publication(s) in Google Scholar
WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. WP1066 can cross the blood-brain barrier[1][2][3][4].
For research use only. We do not sell to patients.
- Purity: 99.53%
- CAS No.: 857064-38-1
- Formula: C17H14BrN3O
- Molecular Weight:356.22
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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) WP1066
More- Cell Metab. 2023 Oct 3;35(10):1688-1703.e10. [Abstract]
- Adv Sci (Weinh). 2025 Apr 25:e2502108. [Abstract]
- J Clin Invest. 2026 Mar 17:e199056. [Abstract]
- J Clin Invest. 2024 Jun 17;134(12):e175033. [Abstract]
- J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]
- Sci Adv. 2024 Mar 22;10(12):eadl0368. [Abstract]
- Adv Healthc Mater. 2024 Jul 19:e2401512. [Abstract]
- Cell Death Dis. 2021 Jun 2;12(6):570. [Abstract]
- Acta Neuropathol. 2021 Sep;142(3):537-564. [Abstract]
- Acta Pharmacol Sin. 2020 Feb;41(2):218-228. [Abstract]
- Free Radic Biol Med. 2024 Aug 28:S0891-5849(24)00630-0. [Abstract]
- Free Radic Biol Med. 2017 Jul:108:542-553. [Abstract]
- J Transl Med. 2019 Apr 2;17(1):107. [Abstract]
- Oncogene. 2026 May;45(19):1840-1855. [Abstract]
- Br J Cancer. 2025 Apr;132(7):599-610. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- OncoImmunology. 2021 Nov 23;10(1):2004659. [Abstract]
- Biochem Pharmacol. 2024 Mar:221:116040. [Abstract]
- Cells. 2024 Dec 26;14(1):10. [Abstract]
- Life Sci. 2025 May 20:123749. [Abstract]
- Cancer Immunol Immunother. 2022 Jun 20. [Abstract]
- Life Sci. 2021 Jan 1;264:118677. [Abstract]
- Int J Mol Sci. 2022 Apr 12;23(8):4277. [Abstract]
- Eur J Pharmacol. 2025 Apr 9:177606. [Abstract]
- Hepatol Commun. 2025 Mar 24;9(4):e0647. [Abstract]
- Exp Neurol. 2025 Dec 31:398:115633. [Abstract]
- FEBS J. 2022 May;289(10):2809-2827. [Abstract]
- Sci Rep. 2025 May 15;15(1):16869. [Abstract]
- J Biol Chem. 2025 Jan 24:108230. [Abstract]
- Oncol Rep. 2021 Jan;45(1):129-138. [Abstract]
- Cell Cycle. 2020 Jun;19(11):1275-1284. [Abstract]
- J Cancer. 2017 Feb 25;8(5):816-824. [Abstract]
- Pflugers Arch. 2024 Dec;476(12):1913-1928. [Abstract]
- Breast Cancer. 2019 Sep;26(5):663-671. [Abstract]
- Cancer Manag Res. 2018 Nov 26:10:6339-6355. [Abstract]
- Biotechnol Lett. 2020 Oct;42(10):2049-2058. [Abstract]
- BMC Pediatr. 2025 Apr 12;25(1):286. [Abstract]
- Biol Pharm Bull. 2023 Aug;46(11):1517-1526. [Abstract]
- Am J Transl Res. 2019 Aug 15;11(8):5212-5226. [Abstract]
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Biological Activity
|
JAK2 |
STAT3 |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
4.2 μM
Compound: WP1066
|
Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
|
[PMID: 34055214] |
| U-266 | IC50 |
1.5 μM
Compound: WP1066
|
Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
|
[PMID: 22036213] |
| U-373MG ATCC | IC50 |
3.7 μM
Compound: WP1066
|
Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay
|
[PMID: 22036213] |
| U-87MG ATCC | IC50 |
5.6 μM
Compound: WP1066
|
Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay
|
[PMID: 22036213] |
WP1066 markedly inhibits the growth of HEL cells in a dose-dependent manner. The IC50 value for inhibition of the proliferation of HEL cells is 2.3 μM. WP1066 inhibits the growth of human HEL cells carrying the JAK2 V617F mutant isoform[1]. Blockade of p-STAT3 with WP1066 enhances the cytotoxic effects of CTX on the tumor. The IC50 doses of WP1066 for B16 cells is 2.43 μM (0.865 μg/mL)[2]. WP1066 inhibits AML blast colony-forming cell proliferation, suppresses normal BM progenitor proliferation at increased concentrations, and inhibits AML colony-forming cell proliferation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
WP1066 shows excellent CNS penetration provided compelling rationale for testing WP1066 against a variety cancer[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 857064-38-1
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Appearance Solid
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Molecular Weight 356.22
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Formula C17H14BrN3O
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Color White to light yellow
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SMILES
O=C(N[C@H](C1=CC=CC=C1)C)/C(C#N)=C/C2=NC(Br)=CC=C2
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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 (39)
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Journal Impact Factor
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Most Recent
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Cell Metab
Neutrophils resist ferroptosis and promote breast cancer metastasis through aconitate decarboxylase 1. [Abstract]2023 Oct 3;35(10):1688-1703.e10. PMID: 37793345 -
Adv Sci (Weinh)
CCDC80 Protects against Aortic Dissection and Rupture by Maintaining the Contractile Smooth Muscle Cell Phenotype. [Abstract]2025 Apr 25:e2502108. PMID: 40278823 -
J Clin Invest
Symbiotic exclusivity between CLOCK and TFPI2 drives stemness and immunosuppression in glioblastoma models. [Abstract]2026 Mar 17:e199056. PMID: 41842961 -
J Clin Invest
STING agonist 8803 reprograms the immune microenvironment and increases survival in preclinical models of glioblastoma. [Abstract]2024 Jun 17;134(12):e175033. PMID: 38941297 -
J Exp Clin Cancer Res
CYP3A5 promotes glioblastoma stemness and chemoresistance through fine-tuning NAD+/NADH ratio. [Abstract]2025 Jan 3;44(1):3. PMID: 39754188 -
Sci Adv
2024 Mar 22;10(12):eadl0368. PMID: 38507500 -
Adv Healthc Mater
Dual-Barb Microneedle with JAK/STAT Inhibitor-Loaded Nanovesicles Encapsulation for Tendinopathy. [Abstract]2024 Jul 19:e2401512. PMID: 39030889 -
Cell Death Dis
SLC7A2 deficiency promotes hepatocellular carcinoma progression by enhancing recruitment of myeloid-derived suppressors cells. [Abstract]2021 Jun 2;12(6):570. PMID: 34108444 -
Acta Neuropathol
Targeting cancer stem cells in medulloblastoma by inhibiting AMBRA1 dual function in autophagy and STAT3 signalling. [Abstract]2021 Sep;142(3):537-564. PMID: 34302498 -
Acta Pharmacol Sin
ZYZ-803, a novel hydrogen sulfide-nitric oxide conjugated donor, promotes angiogenesis via cross-talk between STAT3 and CaMKII. [Abstract]2020 Feb;41(2):218-228. PMID: 31316179
WP1066 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Feb;41(2):218-228. [Abstract]
HUVECs are pretreated with WP1066 for 1 h, followed by ZYZ-803 (1 μM) for 30 min. Protein levels are assessed by Western blot.
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Free Radic Biol Med
Mechanism of cigarette smoke in promoting small airway remodeling in mice via STAT 3 / PINK 1-Parkin / EMT. [Abstract]2024 Aug 28:S0891-5849(24)00630-0. PMID: 39214258 -
Free Radic Biol Med
SERPINB1 ameliorates acute lung injury in liver transplantation through ERK1/2-mediated STAT3-dependent HO-1 induction. [Abstract]2017 Jul:108:542-553. PMID: 28427999
WP1066 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2017 Jul:108:542-553. [Abstract]
The role of STAT3 in SERPINB1-mediated protecting ALI in OALT is further confirmed by using STAT3 specific inhibitor WP1066. post-OALT lung STAT3 activation is significantly increased evidenced by elevated phosphorylation of STAT3 at site727 and site705 (P<0.01 vs sham), which are associated with enhanced HO-1 protein expression.
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J Transl Med
FNDC5 attenuates obesity-induced cardiac hypertrophy by inactivating JAK2/STAT3-associated inflammation and oxidative stress. [Abstract]2019 Apr 2;17(1):107. PMID: 30940158 -
Oncogene
HERC1 oncogene enhances stemness and tumorigenic potential in CD44+-derived organoids of head and neck squamous cell carcinoma through IL-6/STAT3 signaling. [Abstract]2026 May;45(19):1840-1855. PMID: 41965446 -
Br J Cancer
Apolipoprotein D is crucial for promoting perineural invasion in salivary adenoid cystic carcinoma. [Abstract]2025 Apr;132(7):599-610. PMID: 39962257 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
OncoImmunology
Chronic stress promotes breast carcinoma metastasis by accumulating myeloid-derived suppressor cells through activating β-adrenergic signaling. [Abstract]2021 Nov 23;10(1):2004659. PMID: 34858728 -
Biochem Pharmacol
WP1066, a small molecule inhibitor of STAT3, chemosensitizes paclitaxel-resistant ovarian cancer cells to paclitaxel by simultaneously inhibiting the activity of STAT3 and the interaction of STAT3 with Stathmin. [Abstract]2024 Mar:221:116040. PMID: 38311257 -
Cells
Nootkatone Derivative Nootkatone-(E)-2-iodobenzoyl hydrazone Promotes Megakaryocytic Differentiation in Erythroleukemia by Targeting JAK2 and Enhancing JAK2/STAT3 and PKCδ/MAPK Crosstalk. [Abstract]2024 Dec 26;14(1):10. PMID: 39791711 -
Life Sci
PSME2 promotes malignant progression through autophagy modulation via IL-6/STAT3 signaling pathway in esophageal squamous cell carcinoma. [Abstract]2025 May 20:123749. PMID: 40404117 -
Cancer Immunol Immunother
Myeloid-derived suppressor cells cross-talk with B10 cells by BAFF/BAFF-R pathway to promote immunosuppression in cervical cancer. [Abstract]2022 Jun 20. PMID: 35725835 -
Life Sci
Interleukin-22 regulating Kupffer cell polarization through STAT3/Erk/Akt crosstalk pathways to extenuate liver fibrosis. [Abstract]2021 Jan 1;264:118677. PMID: 33129875 -
Int J Mol Sci
2022 Apr 12;23(8):4277. PMID: 35457095 -
Eur J Pharmacol
Carnosol inhibits influenza A virus by disrupting the viral envelope and interfering with Jak2/STAT3 signaling pathway. [Abstract]2025 Apr 9:177606. PMID: 40216182 -
Hepatol Commun
PRMT1-mediated modification of H4R3me2a promotes liver cancer progression by enhancing the transcriptional activity of SOX18. [Abstract]2025 Mar 24;9(4):e0647. PMID: 40130992 -
Exp Neurol
Apelin-13 attenuates microglia-mediated neuroinflammation following intracerebral hemorrhage via targeting JAK2/STAT3 signaling pathway. [Abstract]2025 Dec 31:398:115633. PMID: 41482108 -
FEBS J
TNF-α/ENO1 signaling facilitates testicular phagocytosis by directly activating Elmo1 gene expression in mouse Sertoli cells. [Abstract]2022 May;289(10):2809-2827. PMID: 34919331 -
Sci Rep
Interleukin-7 enhances recruitment of MDSCs by regulating MCP-1 via JAK1/STAT3 signaling pathway in non-small cell lung cancer. [Abstract]2025 May 15;15(1):16869. PMID: 40374882 -
J Biol Chem
Exogenous L-fucose attenuates depression induced by chronic unpredictable stress: implicating core fucosylation has an antidepressant potential. [Abstract]2025 Jan 24:108230. PMID: 39864626 -
Oncol Rep
SOX12 contributes to the activation of the JAK2/STAT3 pathway and malignant transformation of esophageal squamous cell carcinoma. [Abstract]2021 Jan;45(1):129-138. PMID: 33416144 -
Cell Cycle
YAP1, targeted by miR-375, enhanced the pro-angiogenesis of airway smooth muscle cells in asthma via STAT3 activation. [Abstract]2020 Jun;19(11):1275-1284. PMID: 32308108 -
J Cancer
B7-H3 Promotes the Migration and Invasion of Human Bladder Cancer Cells via the PI3K/Akt/STAT3 Signaling Pathway. [Abstract]2017 Feb 25;8(5):816-824. PMID: 28382144
WP1066 purchased from MedChemExpress. Usage Cited in: J Cancer. 2017 Feb 25;8(5):816-824. [Abstract]
The protein expression levels of p-Akt, t-Akt, p-STAT3, t-STAT3, MMP2 and MMP9 are determined via western blotting 48 h after knockdown of B7-H3 and blockade of the PI3K/Akt pathway using LY294002 or the STAT3 pathway using WP1066.
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Pflugers Arch
Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase. [Abstract]2024 Dec;476(12):1913-1928. PMID: 39347835 -
Breast Cancer
PIM1 is responsible for IL-6-induced breast cancer cell EMT and stemness via c-myc activation. [Abstract]2019 Sep;26(5):663-671. PMID: 30989585 -
Cancer Manag Res
Uridine-cytidine kinase 2 promotes metastasis of hepatocellular carcinoma cells via the Stat3 pathway. [Abstract]2018 Nov 26:10:6339-6355. PMID: 30568496
WP1066 purchased from MedChemExpress. Usage Cited in: Cancer Manag Res. 2018 Nov 26:10:6339-6355. [Abstract]
Western blotting analysis: treatment with the Stat3 inhibitor WP1066 neutralizes the up-regulation of MMP2 and MMP9 and reverses the EMT progression caused by the overexpression of Uck2 in Bel-7402 cells.
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Biotechnol Lett
Piperine inhibits colorectal cancer migration and invasion by regulating STAT3/Snail-mediated epithelial-mesenchymal transition. [Abstract]2020 Oct;42(10):2049-2058. PMID: 32500474 -
BMC Pediatr
Butyrate inhibits histone deacetylase 2 expression to alleviate liver fibrosis in biliary atresia. [Abstract]2025 Apr 12;25(1):286. PMID: 40221650 -
Biol Pharm Bull
Anti-neuroinflammatory Effects of Active Compound SPA1413 via Suppression of the MAPK and JAK/STAT Signaling Pathways. [Abstract]2023 Aug;46(11):1517-1526. PMID: 37914355 -
Am J Transl Res
Resveratrol improves cardiac function by promoting M2-like polarization of macrophages in mice with myocardial infarction. [Abstract]2019 Aug 15;11(8):5212-5226. PMID: 31497235
Solvent & Solubility
DMSO : ≥ 44 mg/mL (123.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 16.67 mg/mL (46.80 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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: ≥ 5 mg/mL (14.04 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal experiments:
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-
-
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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
Briefly, fresh low-density peripheral blood cells and various cell lines at the logarithmic phase of their growth are washed twice in RPMI 1640 containing 10% FCS and counted in a hemocytometer. Cell viability is assessed by the trypan blue (0.1%) staining method. Equal numbers of viable cells (5×104 per well) are incubated in a total volume of 100 μL of RPMI 1640 supplemented with 10% FCS alone or with WP1066 at increasing concentrations; the incubations are continued for up to 72 h in 96-well flat-bottomed plates at 37°C in a humidified 5% CO2 atmosphere. Experiments for each condition are done in triplicate. After incubation, 20 μL of CellTiter96 One Solution Reagent are added to each well. The plates are then incubated for an additional 60 min at 37°C in a humidified 5% CO2 atmosphere. Immediately after incubation, absorbance is read using a 96-well plate reader at a wavelength of 490 nm.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To ascertain the inhibition of the immune populations within the spleen and peripheral blood compartments, tumor-bearing mice are treated with CTX, WP1066, or CTX in combination with WP1066, for 14 days. Single-cell suspensions are prepared from spleens and the peripheral blood of mice and single cells are surface-stained with FITC-conjugated anti-CD4 (L3T4) or PE-conjugated anti-CD8 (53-6.7) and are intracellularly stained with APC-conjugated-FoxP3 (clone FJK-16s). The cell number of CD4+ and CD8+ T cells in the peripheral blood is counted based on positive surface staining of the respective markers relative to the total cell count of PBMCs. The percentage of FoxP3+ Tregs is calculated within the peripheral blood and within the CD4 compartment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Verstovsek S, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res, 2008, (3), 788-796. [Content Brief]
[2]. Hatiboglu MA, et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of WP1066 in murine melanoma models. Int J Cancer, 2012, 131(1), 8-17 [Content Brief]
[3]. Ferrajoli A, et al. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res, 2007, 67(23), 11291-11299. [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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.8073 mL | 14.0363 mL | 28.0725 mL | 70.1813 mL |
| 5 mM | 0.5615 mL | 2.8073 mL | 5.6145 mL | 14.0363 mL | |
| 10 mM | 0.2807 mL | 1.4036 mL | 2.8073 mL | 7.0181 mL | |
| 15 mM | 0.1872 mL | 0.9358 mL | 1.8715 mL | 4.6788 mL | |
| 20 mM | 0.1404 mL | 0.7018 mL | 1.4036 mL | 3.5091 mL | |
| 25 mM | 0.1123 mL | 0.5615 mL | 1.1229 mL | 2.8073 mL | |
| 30 mM | 0.0936 mL | 0.4679 mL | 0.9358 mL | 2.3394 mL | |
| 40 mM | 0.0702 mL | 0.3509 mL | 0.7018 mL | 1.7545 mL | |
| DMSO | 50 mM | 0.0561 mL | 0.2807 mL | 0.5615 mL | 1.4036 mL |
| 60 mM | 0.0468 mL | 0.2339 mL | 0.4679 mL | 1.1697 mL | |
| 80 mM | 0.0351 mL | 0.1755 mL | 0.3509 mL | 0.8773 mL | |
| 100 mM | 0.0281 mL | 0.1404 mL | 0.2807 mL | 0.7018 mL |