2. Stem Cell/Wnt Protein Tyrosine Kinase/RTK
  3. YAP VEGFR Hippo (MST)
  4. VT3989

VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors.

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VT3989

VT3989 화학구조

CAS No. : 2506273-81-8

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

VT3989 Related Antibodies

Top Publications Citing Use of Products

View All YAP Isoform Specific Products:

View All Isoforms
YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All Hippo (MST) Isoform Specific Products:

View All Isoforms
MST1 MST2 MST3 MST4

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors[1][2][3][4].
IC50 & Target

YAP/TAZ

 

In Vitro

VT3989 exhibits strong to very strong synergy with osimertinib in cell proliferation assays using EGFR mutant NSCLC cell lines[3].
VT3989, a TEAD central pocket inhibitor, reduces expression of TEAD target genes and is cytotoxic to NF2-deficient IOMM-Lee and MG309 meningioma cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

VT3989 Related Antibodies
In Vivo

VT3989 (30 mg/kg; p.o.; daily; 21 days) reverses elevated Vegfa expression and reduces Schwann cell-specific Vegfa signal in a mouse model of merlin-deficient schwannoma[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Periostin-CRE;NF2fl/fl mice (5-month-old; male and female; age-matched NF2fl/fl-CRE- littermate controls; biallelic NF2/merlin loss in Schwann cells)[2]
Dosage: 30 mg/kg
Administration: p.o.; daily; 21 days
Result: Reversed the 2-fold increase in normalized Vegfa expression seen in vehicle-treated NF2fl/fl-Cre+ mice, returning levels to those seen in NF2fl/fl-Cre- control mice.
Reduced Schwann cell-associated Vegfa signal in dorsal root ganglia of treated mice, with no change in neuron-associated Vegfa signal.
분자량

389.37

화학식

C21H18F3NO3
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

OC[C@@H](C)NC(C(C=C1)=CC2=C1C(OC3=CC=C(C=C3)C(F)(F)F)=CC=C2)=O
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : ≥ 100 mg/mL (256.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5683 mL 12.8413 mL 25.6825 mL
5 mM 0.5137 mL 2.5683 mL 5.1365 mL
View the 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.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.42 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.42 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
순도&문서

Purity: 99.61%

SDS (252 KB)

COA (246 KB) HNMR (273 KB) RP-HPLC (252 KB) MS (69 KB)

Handling Instructions (2659 KB)
References

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 2.5683 mL 12.8413 mL 25.6825 mL 64.2063 mL
5 mM 0.5137 mL 2.5683 mL 5.1365 mL 12.8413 mL
10 mM 0.2568 mL 1.2841 mL 2.5683 mL 6.4206 mL
15 mM 0.1712 mL 0.8561 mL 1.7122 mL 4.2804 mL
20 mM 0.1284 mL 0.6421 mL 1.2841 mL 3.2103 mL
25 mM 0.1027 mL 0.5137 mL 1.0273 mL 2.5683 mL
30 mM 0.0856 mL 0.4280 mL 0.8561 mL 2.1402 mL
40 mM 0.0642 mL 0.3210 mL 0.6421 mL 1.6052 mL
50 mM 0.0514 mL 0.2568 mL 0.5137 mL 1.2841 mL
60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0701 mL
80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8026 mL
100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6421 mL
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VT3989 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VT39892506273-81-8VT 3989VT-3989YAPVEGFRHippo (MST)Yes-associated proteinVascular endothelial growth factor receptormerlin-depleted Schwann cellshuman-derived schwannoma cellsYAP/TAZ-TEAD complexepithelioid hemangioendotheliomamalignant pleural mesotheliomaneurofibromatosis type 2vestibular schwannomaNF2-loss meningioma cellsTEAD transcription factorsEGFR mutant non-small cell lung cancerInhibitorinhibitorinhibit

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상품명:
VT3989
Cat. No.:
HY-400902
수량:
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SAFETY DATA SHEET (SDS)

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