| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC TEAD/IAP degrader-1 (compound A536) (20 hours) can degrade HiBiT-TEAD1 in NCI-H2052 cells, with a DC50 of 233 nM and a Dmax of 67% [1]. PROTAC TEAD/IAP degrader-1 (20 hours) can degrade endogenous TEAD1 in NCI-H2052 cells, with a DC50 of 110 nM and a Dmax of 51% [1]. PROTAC TEAD/IAP degrader-1 (20 hours) can weakly degrade endogenous TEAD4 in NCI-H2052 cells, with a DC50 of 990 nM and a Dmax of 24%, indicating that its selectivity for TEAD1 is higher than that for TEAD4 [1]. PROTAC TEAD/IAP degrader-1 (18 h) preferentially degraded HiBiT-TEAD1 in NCI-H226 cells after 18 hours of treatment, with weak activity against HiBiT-TEAD3 (Dmax of 16%) and extremely low activity against HiBiT-TEAD2 and HiBiT-TEAD4 [1]. PROTAC TEAD/IAP degrader-1 (2 h) bound to intracellular cIAP1 in HEK293T cells, with a live-cell IC50 of 327 nM and moderate intracellular bioavailability [1]. PROTAC TEAD/IAP degrader-1 (2 h) bound to intracellular XIAP in HEK293T cells, with an IC50 of 701 nM [1]. PROTAC TEAD/IAP degrader-1 (4 h) promoted the formation of the cIAP1-TEAD1 ternary complex in NCI-H2052 cells, with an ECmax of 1920 nM and an Emax of 73 mBU[1]. PROTAC TEAD/IAP degrader-1 (4 h) promoted the formation of the XIAP-TEAD1 ternary complex in NCI-H2052 cells, with an ECmax of 6860 nM and an Emax of 22 mBU[1]. PROTAC TEAD/IAP degrader-1 (144 h) inhibited the proliferation of Hippo-dependent mesothelioma cell lines (NCI-H226, NCI-H2052, ZL55) and Hippo-independent NCI-H520 cells, with IC50 values ranging from 386 nM to 1250 nM[1]. PROTAC TEAD/IAP degrader-1 (48 hours) downregulated CTGF mRNA (TEAD target gene) in Hippo-dependent mesothelioma cell lines with IC50 values ranging from 170 nM to 380 nM and Emax values ranging from 87% to 93% [1].
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|---|---|
| References |
| Molecular Formula |
C51H48F3N11O3S
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|---|---|
| Molecular Weight |
952.06
|
| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CN[C@H](C(NC1=CC=C(C(C#CC2=CN=CS2)=N1)C3=C(N(N=C3C)CC(N4CC5(C4)CCN(CC5)C6=CC=CC(CNC(C7=CC8=CC=CC(C9=CC=C(C=C9)C(F)(F)F)=C8N=C7)=O)=N6)=O)C)=O)C
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.0504 mL | 5.2518 mL | 10.5035 mL | |
| 5 mM | 0.2101 mL | 1.0504 mL | 2.1007 mL | |
| 10 mM | 0.1050 mL | 0.5252 mL | 1.0504 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
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