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| 5mg |
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| 25mg |
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DT2216 (DT-2216; DT 2216) is a novel and potent degrader of B-cell lymphoma extra large (BCL-XL) based on proteolysis-targeting chimera (PROTAC) technology. By attracting BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation via the proteasome-dependent pathway, DT2216 exhibits anti-leukemia and anticancer properties.
| Targets |
BCL-XL
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|---|---|
| ln Vitro |
DT2216 is a Von Hippel-Lindau (VHL) E3 ligase-targeted BCL-XL proteolysis targeting chimera (PROTAC) that directs BCL-XL for degradation. Because VHL is poorly expressed in platelets, DT2216 is significantly less toxic to platelets than ABT263, making it more effective against a variety of BCL-XL-dependent leukemia and cancer cells. [1]
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| ln Vivo |
As a single agent or in combination with other chemotherapeutic drugs, DT2216 effectively slows the growth of several xenograft tumors in vivo without significantly increasing thrombocytopenia.[1]
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| Cell Assay |
The indicated concentrations of DT2216 or ABT263 are then applied to MOLT-4 cells for 24 hours after they have been seeded in 60 mm dishes (2.5 × 106 cells in 5 mL complete cell culture medium/dish). A freeze-thaw cycle in an ice-ethanol bath or a 30-minute incubation on ice are both effective ways to lyse cells in 1X cell lysis buffer.
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| References |
| Molecular Formula |
C₇₇H₉₆CLF₃N₁₀O₁₀S₄
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|---|---|
| Molecular Weight |
1542.36
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| Exact Mass |
1,540.58
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| Elemental Analysis |
C, 59.96; H, 6.27; Cl, 2.30; F, 3.70; N, 9.08; O, 10.37; S, 8.31
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| CAS # |
2365172-42-3
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| Related CAS # |
2365172-42-3;DT2216 HCl; DT2216NC; DT2216-isomer;
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| Appearance |
Solid powder
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| SMILES |
CC1=C(SC=N1)C2=CC=C(C=C2)[C@H](C)NC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)CCCCCC(=O)N4CCN(CC4)CC[C@H](CSC5=CC=CC=C5)NC6=C(C=C(C=C6)S(=O)(=O)NC(=O)C7=CC=C(C=C7)N8CCN(CC8)CC9=C(CCC(C9)(C)C)C1=CC=C(C=C1)Cl)S(=O)(=O)C(F)(F)F)O
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| InChi Key |
PXVFFBGSTYQHRO-REQIQPEASA-N
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| InChi Code |
InChI=1S/C77H96ClF3N10O10S4/c1-51(53-18-20-55(21-19-53)70-52(2)82-50-103-70)83-73(96)66-44-61(92)48-91(66)74(97)71(75(3,4)5)85-68(93)16-12-9-13-17-69(94)90-42-36-87(37-43-90)35-33-59(49-102-62-14-10-8-11-15-62)84-65-31-30-63(45-67(65)104(98,99)77(79,80)81)105(100,101)86-72(95)56-24-28-60(29-25-56)89-40-38-88(39-41-89)47-57-46-76(6,7)34-32-64(57)54-22-26-58(78)27-23-54/h8,10-11,14-15,18-31,45,50-51,59,61,66,71,84,92H,9,12-13,16-17,32-44,46-49H2,1-7H3,(H,83,96)(H,85,93)(H,86,95)/t51-,59+,61+,66-,71+/m0/s1
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| Chemical Name |
(2S,4R)-1-[(2S)-2-[[7-[4-[(3R)-3-[4-[[4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]benzoyl]sulfamoyl]-2-(trifluoromethylsulfonyl)anilino]-4-phenylsulfanylbutyl]piperazin-1-yl]-7-oxoheptanoyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
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| Synonyms |
DT2216 HCl; DT-2216; DT 2216; DT2216
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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) |
DMSO: ~100 mg/mL (~64.8 mM)
Ethanol: ~100 mg/mL (~64.8 mM) |
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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 | 0.6484 mL | 3.2418 mL | 6.4836 mL | |
| 5 mM | 0.1297 mL | 0.6484 mL | 1.2967 mL | |
| 10 mM | 0.0648 mL | 0.3242 mL | 0.6484 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04886622 | Recruiting | Drug: DT2216 | Solid Tumor Hematologic Malignancy |
Dialectic Therapeutics, Inc | August 25, 2021 | Phase 1 |
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