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| Other Sizes |
Purity: ≥98%
ZXH-3-26 is a novel, potent and selective degrader of BRD4 with a DC50/5h (half-maximal degradation after 5 hours of treatment) of ~ 5 nM. Heterobifunctional small-molecule degraders that induce protein degradation through ligase-mediated ubiquitination have shown considerable promise as a new pharmacological modality.
| ln Vitro |
The first small chemical that permits medicines to inhibit BRD4 without substantially inhibiting or degrading BRD2/3 is ZXH-3-26 [1]. ZXH-3-26 degrades endogenous BRD4 with equal efficacy to the best pan-BET degrader, dBET6, according to the first immunoblot investigation on BRD4 only at a dose of 10 μM. Additionally, BRD2/ZXH-3-26 participates in CRBN in a distinct conformation[1]. 3As of right now[1].
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| References |
[1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.
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| Molecular Formula |
C38H37CLN8O7S
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|---|---|
| Molecular Weight |
785.2678
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| CAS # |
2243076-67-5
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| Related CAS # |
2243076-67-5;2307475-86-9 (TFA);ZXH-3-26 HCl;
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(OC)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C(NCCCCCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)S3)C(C7=CC=C(Cl)C=C7)=N1
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| InChi Key |
KLLGWPDWPSUTCL-QBHOUYDASA-N
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| InChi Code |
InChI=1S/C39H39ClN8O7S/c1-20-30-32(22-11-13-23(40)14-12-22)43-26(19-29(50)55-3)34-46-45-21(2)47(34)39(30)56-33(20)36(52)42-18-7-5-4-6-17-41-25-10-8-9-24-31(25)38(54)48(37(24)53)27-15-16-28(49)44-35(27)51/h8-14,26-27,41H,4-7,15-19H2,1-3H3,(H,42,52)(H,44,49,51)/t26-,27?/m0/s1
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| Chemical Name |
Methyl 2-((6S)-4-(4-chlorophenyl)-2-((6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)carbamoyl)-3,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
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| Synonyms |
ZXH326; ZXH 3 26; ZXH-326; ZXH-3-26
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~200 mg/mL (~254.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2734 mL | 6.3672 mL | 12.7345 mL | |
| 5 mM | 0.2547 mL | 1.2734 mL | 2.5469 mL | |
| 10 mM | 0.1273 mL | 0.6367 mL | 1.2734 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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