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Purity: ≥98%
WP1066, an AG49 derivative, is a novel and potent inhibitor of Janus kinases-JAK2 and STAT3 with potential antitumor activity. It inhibits JAK2 and STAT3 with IC50s of 2.30 μM and 2.43 μM in HEL cells. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.
| ln Vitro |
The proliferation of HEL cells was greatly suppressed in a dose-dependent manner by WP10666. 2.3 μM is the IC50 value for suppressing HEL cell growth. Human HEL cells with the JAK2 V617F mutant isoform cannot proliferate when WP1066 is present [1]. When WP1066 was used to block p-STAT3, the cytotoxic effect of CTX on tumors was increased. On B16 cells, WP1066's IC50 dosage is 2.43 μM (0.865 μg/mL)[2]. At high concentrations, WP1066 suppresses the growth of normal BM progenitor cells, suppresses the proliferation of AML blast colony-forming cells, and suppresses the proliferation of AML colony-forming cells [3].
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| ln Vivo |
In the tumor microenvironment, WP1066 (30 mg/kg, og) had additive effects on CTX-induced p-STAT3 pathway inhibition [2].
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| Additional Infomation |
WP1066 has been used in trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.
STAT3 Inhibitor WP1066 is an orally bioavailable, small molecule inhibitor of signaling transducer and activator 3 (STAT3), with potential antineoplastic and immunomodulatory activities. Upon administration, STAT3 inhibitor WP1066 blocks the intranuclear translocation of p-STAT, thereby suppressing STAT3 signaling and decreasing the levels of downstream products including c-Myc. Additionally, WP1066 may upregulate costimulatory molecules including CD80 and CD86 on human microglia, and reverse glioma cancer stem cell (gCSC)-mediated innate and adaptive immune suppression allowing for the restoration of antitumor effector immune responses. The STAT3 pathway is overly active in many cancer types and is implicated in CSC-mediated growth, recurrence and resistance to conventional chemotherapies. |
| Molecular Formula |
C17H14BRN3O
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| Molecular Weight |
356.22
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| Exact Mass |
355.032
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| CAS # |
857064-38-1
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| Related CAS # |
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| PubChem CID |
11210478
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
569.9±50.0 °C at 760 mmHg
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| Flash Point |
298.5±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
2.95
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
462
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H](C1=CC=CC=C1)NC(=O)/C(=C/C2=NC(=CC=C2)Br)/C#N
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| InChi Key |
VFUAJMPDXIRPKO-LQELWAHVSA-N
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| InChi Code |
InChI=1S/C17H14BrN3O/c1-12(13-6-3-2-4-7-13)20-17(22)14(11-19)10-15-8-5-9-16(18)21-15/h2-10,12H,1H3,(H,20,22)/b14-10+/t12-/m0/s1
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| Chemical Name |
(S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide
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| Synonyms |
WP-1066; WP 1066; WP1066
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8073 mL | 14.0363 mL | 28.0725 mL | |
| 5 mM | 0.5615 mL | 2.8073 mL | 5.6145 mL | |
| 10 mM | 0.2807 mL | 1.4036 mL | 2.8073 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04334863 | Completed | Drug: WP1066 | Brain Tumor Medulloblastoma |
Emory University | May 4, 2020 | Phase 1 |
| NCT01904123 | Completed | Other: Pharmacological Study Drug: STAT3 Inhibitor WP1066 |
Metastatic Melanoma Recurrent Brain Neoplasm |
M.D. Anderson Cancer Center | July 13, 2018 | Phase 1 |
| NCT05879250 | Not yet recruiting | Procedure: Biospecimen Collection Procedure: Magnetic Resonance Imaging |
Glioblastoma, IDH-Wildtype MGMT-Unmethylated Glioblastoma |
Northwestern University | December 27, 2024 | Phase 2 |
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WP1066 downregulates HIF1α and HIF2α expression and reduces VEGF production in renal cancer cells.Br J Cancer.2010 May 25;102(11):1592-9. |
WP1066 inhibits tumour growth in the murine xenograft model of Caki-1 cells.Br J Cancer.2010 May 25;102(11):1592-9. |
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