| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| ln Vivo |
In a syngeneic mouse model of Wnt1 tumors, E-7386, an oral active modulator of CBP/β-catenin, increases the anti-tumor effectiveness of anti-PD-1 mAb and causes T cell infiltration into tumors. In the Wnt1 model, E-7386 shows strong anti-tumor efficacy. T cell infiltration into the tumor was minimal in the vehicle control group, but it was evident in the E-7386 therapy group [1].
|
|---|---|
| References | |
| Additional Infomation |
E7386, a CBP/β-catenin modulator, is an orally bioavailable, classic Wnt/β-catenin signaling pathway-specific inhibitor with potential antitumor activity. After oral administration, E7386 inhibits β-catenin and prevents its interaction with its transcriptional coactivator CREB (cAMP response element-binding protein) (CBP). This prevents the binding of β-catenin/CBP to WRE (Wnt response element) and inhibits the transcriptional activation of multiple target genes in the Wnt/β-catenin signaling pathway, thereby suppressing the expression of many Wnt-related pro-survival proteins and inhibiting tumor cell growth. The Wnt/β-catenin signaling pathway regulates cell morphology, motility, and proliferation; abnormal regulation of this pathway leads to tumor cell proliferation. β-catenin is frequently mutated in various tumors.
|
| Molecular Formula |
C39H48FN9O4
|
|---|---|
| Molecular Weight |
725.854731559753
|
| Exact Mass |
725.381
|
| CAS # |
1799824-08-0
|
| PubChem CID |
91810345
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
53
|
| Complexity |
1280
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
N1(CC=C)CC(=O)N2[C@@H](CC3=CC=C(O)C=C3F)C(=O)N(CC3=NC(N4CC(N5CCN(CC)CC5)C4)=CC=C3)C[C@]2([H])N1C(NCC1=CC=CC=C1)=O
|
| InChi Key |
ZGNKNLOBYFTGRG-GIWKVKTRSA-N
|
| InChi Code |
InChI=1S/C39H48FN9O4/c1-3-15-47-27-37(51)48-34(20-29-13-14-32(50)21-33(29)40)38(52)46(26-36(48)49(47)39(53)41-22-28-9-6-5-7-10-28)23-30-11-8-12-35(42-30)45-24-31(25-45)44-18-16-43(4-2)17-19-44/h3,5-14,21,31,34,36,50H,1,4,15-20,22-27H2,2H3,(H,41,53)/t34-,36-/m0/s1
|
| Chemical Name |
(6S,9aS)-N-benzyl-8-[[6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl]methyl]-6-[(2-fluoro-4-hydroxyphenyl)methyl]-4,7-dioxo-2-prop-2-enyl-3,6,9,9a-tetrahydropyrazino[2,1-c][1,2,4]triazine-1-carboxamide
|
| 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 : ~125 mg/mL (~172.21 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3777 mL | 6.8885 mL | 13.7770 mL | |
| 5 mM | 0.2755 mL | 1.3777 mL | 2.7554 mL | |
| 10 mM | 0.1378 mL | 0.6888 mL | 1.3777 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
