| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
PROTAC RIPK1 degrader-1 (compound 225-5) (0-1 μM, 1-20 h) induced RIPK1 degradation in HEK-293T-RIPK1-HiBiT (DC50 < 0.1 nM, Dmax = 93 %), A375 (DC50 = 41 nM, Dmax = 97 %), B16F10 (DC50 = 91 nM, Dmax = 92 %), PC3, LNCap, MCF7, NOMO1, RS$;11, and U87 cells by binding to RIPK1, VHL, proteasome, and Cullin-RING E3 ligase complex [1].
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| ln Vivo |
PROTAC RIPK1 degrader-1 (compound 225-5) (10-50 mg/kg, intraperitoneal/intravenous injection, twice daily/once daily for 3-11 days) reduced RIPK1 levels in the B16F10 C57BL/6 mouse model [1]. PROTAC RIPK1 degrader-1 (10-20 mg/kg, intraperitoneal injection, once daily for 3-11 days) reduced RIPK1 levels in the humanized A375 melanoma NSG mouse model [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: A375, B16F10, PC3, LNCap, MCF7, NOMO1, RS$;11, U87 cells Test concentrations: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM Incubation Duration: 1 hour, 2 hours, 4 hours, 8 hours, 16 hours, 20 hours Experimental Results: Induced RIPK1 degradation. |
| Animal Protocol |
Animal/Disease Models:B16F10 (0.3 M) C57BL/6 mouse model [1]
Doses: 50 mg/kg / 10 mg/kg Route of Administration: Intraperitoneal injection, twice daily for 3 consecutive days / Intravenous injection, twice daily for 3 consecutive days Experimental Results: RIPK1 levels decreased. Animal/Disease Models:Humanized (PBMC, 1 × 107) A375 (5 M) melanoma NSG mouse model [1] Doses: 10 mg/kg, 20 mg/kg Route of Administration: Intraperitoneal injection, once daily for 3 consecutive days Experimental Results: RIPK1 levels decreased. Animal/Disease Models:B16F10 (0.3 M) syngeneic C57BL/6 mouse model [1] Doses: 40 mg/kg + 20 mg/kg Route of Administration: Intraperitoneal injection, once daily for 3 days + once daily for 8 days Experimental Results: When used in combination with radiotherapy, it can delay tumor growth and extend median survival from 19 days to 24 days. Animal/Disease Models:A375 (1 M) humanized (PBMC, 1 × 107) NSG mouse model [1] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection, once daily for 11 days Experimental Results: When used in combination with radiotherapy, tumor volume was reduced by 89%. |
| References |
| Molecular Formula |
C69H85N13O6S2
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|---|---|
| Molecular Weight |
1256.63
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(N1CCC(CC1)CN2CCC(CN3CCN(CC(N[C@H](C(N4[C@H](C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)CC3)CC2)CN7C=C(C=N7)C8=CN=C(N)C9=C8SC=C9C%10=CC=C%11N(C(CC%12=CC=CC=C%12)=O)CCC%11=C%10
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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 | 0.7958 mL | 3.9789 mL | 7.9578 mL | |
| 5 mM | 0.1592 mL | 0.7958 mL | 1.5916 mL | |
| 10 mM | 0.0796 mL | 0.3979 mL | 0.7958 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.
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