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| 5mg |
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| 25mg |
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Purity: ≥98%
AZD4320 is a novel, potent BH3-mimic and dual inhibitor of BCL2/BCLxL with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively. Despite recent therapeutic advancements, the prognosis for diffuse large B-cell lymphomas (DLBCLs) that concurrently overexpress c-MYC and BCL2, also known as double hit lymphoma (DHL) and double expressing lymphoma (DEL), is still poor. By increasing the number of cells going through apoptosis in all three of the tested cell lines, AZD4320 and AZD5153 had an antitumor effect that was primarily synergistic. These findings support the dual targeting of BRD4 and BCL2 by AZD5153 and AZD4320 as a therapeutic approach against DHL and DEL.
| Targets |
BCL2 (IC50 = 17 nM); BCLxL (IC50 = 17 nM)
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|---|---|
| ln Vitro |
AZD4320 potently enhances the antitumor effect of AZD5153 in double expressing lymphoma (DEL)- and double hit lymphoma (DHL)-derived cell lines in a dose-dependent manner. On DEL- and DHL-derived cell lines, AZD4320 primarily exhibits synergistic and at least additive growth inhibitory effects, and it significantly increases the number of cells undergoing apoptosis in all three cell lines[1].
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| Cell Assay |
KPUM-MS3 and KPUM-UH1 are two DEL-derived cell lines, and STR-428 is a DHL-derived cell line. Cells are treated with five concentrations of AZD4320 (0.25, 0.5, 1.0, 2.0, and 4.0IC50) for 72 hours, and then the results are measured using a modified MTT assay[1].
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| References |
| Molecular Formula |
C45H48CLF3N4O7S3
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|---|---|
| Molecular Weight |
945.528437614441
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| Exact Mass |
944.23
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| Elemental Analysis |
C, 57.16; H, 5.12; Cl, 3.75; F, 6.03; N, 5.93; O, 11.84; S, 10.17
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| CAS # |
1357576-48-7
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| Related CAS # |
1357576-49-8 (formate);1357576-48-7;
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| PubChem CID |
86661883
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| Appearance |
White to off-white solid powder
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| LogP |
9.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
63
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| Complexity |
1630
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN(CC[C@H](CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCC(CC4)[C@H](C5=CC=CC=C5C6=CC=C(C=C6)Cl)O)S(=O)(=O)C(F)(F)F)CCO
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| InChi Key |
UNEJSHNDABUZNY-UJNHCCGESA-N
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| InChi Code |
InChI=1S/C45H48ClF3N4O7S3/c1-52(27-28-54)24-23-35(30-61-37-7-3-2-4-8-37)50-41-20-19-38(29-42(41)62(57,58)45(47,48)49)63(59,60)51-44(56)33-13-17-36(18-14-33)53-25-21-32(22-26-53)43(55)40-10-6-5-9-39(40)31-11-15-34(46)16-12-31/h2-20,29,32,35,43,50,54-55H,21-28,30H2,1H3,(H,51,56)/t35-,43-/m1/s1
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| Chemical Name |
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[2-hydroxyethyl(methyl)amino]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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| Synonyms |
AZD4320; AZD-4320; AZD 4320
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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 (~105.8 mM）
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (6.61 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 62.5 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 | 1.0576 mL | 5.2880 mL | 10.5761 mL | |
| 5 mM | 0.2115 mL | 1.0576 mL | 2.1152 mL | |
| 10 mM | 0.1058 mL | 0.5288 mL | 1.0576 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 |
| NCT04214093 | Terminated | Drug: AZD0466 | Lymphoma Multiple Myeloma Advanced Solid Tumors |
AstraZeneca | December 16, 2019 | Phase 1 |
| NCT05205161 | Terminated | Drug: AZD0466 | Non-Hodgkin Lymphoma | AstraZeneca | July 5, 2022 | Phase 1 Phase 2 |
| NCT04865419 | Terminated | Drug: AZD0466 Drug: Voriconazole |
Haematological Malignancies | AstraZeneca | June 11, 2021 | Phase 1 Phase 2 |
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