| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
YAP/TAZ inhibitor-2 targets the TEAD-YAP/TAZ interaction, which is a key node in the Hippo signaling pathway. YAP and TAZ are transcriptional coactivators that promote cell proliferation and survival. When the Hippo pathway is active, YAP/TAZ are phosphorylated and degraded. In cancer, this pathway is often dysregulated, leading to increased YAP/TAZ activity. By inhibiting the TEAD-YAP/TAZ interaction, the compound blocks the transcription of YAP/TAZ target genes, thereby inhibiting cell proliferation.
|
|---|---|
| ln Vitro |
Compound 5 (YAP/TAZ inhibitor-2; 0–20,000 nM; 24 h) exhibits anti-proliferative activity in NCI-H226 cells, with an IC50 of 5.33 nM [1].
In vitro, YAP/TAZ inhibitor-2 demonstrates potent anti-proliferative activity. It has an EC50 of 3 nM, indicating its high potency in inhibiting the TEAD-YAP/TAZ interaction. Specific cellular assay data, such as effects on the expression of YAP/TAZ target genes, are not detailed in the available sources. |
| ln Vivo |
YAP/TAZ inhibitor-2 (0.5, 2, 5, 50 mg/kg; route; once daily for 28 days) showed anticancer activity during BALB/c nude mice (NCI-H226 xenograft) therapy , and there is no substantial weight loss model [1].
In vivo, YAP/TAZ inhibitor-2 has shown antitumor activity in a BALB/c nude mouse NCI-H226 xenograft model. Oral administration at doses of 0.5, 2, 5, and 50 mg/kg once daily for 28 days demonstrated antitumor activity, with no significant weight loss observed during the treatment period. These findings support its potential as an anticancer agent. |
| Enzyme Assay |
A cell-free assay for YAP/TAZ inhibitor-2 would involve measuring its ability to disrupt the TEAD-YAP/TAZ protein-protein interaction. These assays typically use purified proteins and techniques such as fluorescence polarization, AlphaScreen, or surface plasmon resonance to measure the binding of YAP/TAZ to TEAD in the presence of the compound.
|
| Cell Assay |
Cellular assays for YAP/TAZ inhibitor-2 typically involve assessing its effects on YAP/TAZ-dependent transcription. Cells are treated with the compound, and the expression of YAP/TAZ target genes is measured by qPCR or reporter assays. The compound's anti-proliferative effects are assessed by measuring cell viability or proliferation.
|
| Animal Protocol |
In vivo animal experiments with YAP/TAZ inhibitor-2 were conducted in BALB/c nude mice bearing NCI-H226 xenografts. The compound was administered orally at doses of 0.5, 2, 5, and 50 mg/kg once daily for 28 days. Tumor growth was measured, and antitumor activity was observed. Body weight was monitored, and no significant weight loss was reported.
|
| ADME/Pharmacokinetics |
YAP/TAZ inhibitor-2 has a molecular formula of C19H14F4N4O. It is an orally active compound. Specific pharmacokinetic parameters, such as half-life and bioavailability, are not provided in the available sources. For storage, the powder should be kept at -20°C.
|
| Toxicity/Toxicokinetics |
Toxicity data for YAP/TAZ inhibitor-2 indicate that at the doses tested in the xenograft model (0.5-50 mg/kg), no significant weight loss was observed, suggesting the compound was tolerated. However, comprehensive toxicological profiles are not available. The compound is intended for research use only and is not for human consumption.
|
| References | |
| Additional Infomation |
YAP/TAZ inhibitor-2 (CAS: 2762617-31-0) is a potent and orally active TEAD-YAP/TAZ inhibitor. It has an EC50 of 3 nM and exhibits anti-proliferative and antitumor activity. It is used in cancer research to study the Hippo signaling pathway. It is not an approved drug and is strictly for research purposes.
|
| Molecular Formula |
C19H14F4N4O
|
|---|---|
| Molecular Weight |
390.33
|
| Exact Mass |
390.11
|
| CAS # |
2762617-31-0
|
| PubChem CID |
164885340
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
3.5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
614
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1(CC(C1)N1N=C(C2C=CC(C(F)(F)F)=CC=2)C2=C1N=CC=C2)C(=O)C(F)=C
|
| InChi Key |
GTRCXQAYBUYBBE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H14F4N4O/c1-11(20)18(28)26-9-14(10-26)27-17-15(3-2-8-24-17)16(25-27)12-4-6-13(7-5-12)19(21,22)23/h2-8,14H,1,9-10H2
|
| Chemical Name |
2-fluoro-1-[3-[3-[4-(trifluoromethyl)phenyl]pyrazolo[3,4-b]pyridin-1-yl]azetidin-1-yl]prop-2-en-1-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~256.19 mM)
|
|---|---|
| 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 | 2.5619 mL | 12.8097 mL | 25.6193 mL | |
| 5 mM | 0.5124 mL | 2.5619 mL | 5.1239 mL | |
| 10 mM | 0.2562 mL | 1.2810 mL | 2.5619 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
