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ZBC260 (ZBC-260; BETd-260) is a potent and selective PROTAC-based BET degrader and BET inhibitor as well. It degrades BRD4 protein at concentrations as low as 30 pM in the RS4;11 leukemia cell line and has anticancer activity.
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| ln Vitro |
In the RS4;11 leukemia cells, BETd-260 (ZBC260; Compound 23) can cause the BRD2, BRD3, and BRD4 proteins to degrade at concentrations between 30 and 100 pM. With IC50s of 51 pM and 2.2 nM, respectively, BETd-260 exhibits inhibitory effect against the development of MOLM-13 and RS4;11 leukemia cells. It also promotes apoptosis in both RS4;11 and MOLM-13 cell lines at 3–10 nM[1]. In HCC cells, BETd-260 reciprocally regulates the expression of many apoptotic genes, i.e., upregulating the expression of pro-apoptotic Bad and downregulating the expression of anti-apoptotic Mcl-1, Bcl-2, c-Myc, and XIAP[2].
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| ln Vivo |
BETd-260 (5 mg/kg, intravenous, every other day, three times a week for three weeks) causes minimal body weight loss or other symptoms of toxicity in mice bearing RS4;11 xenograft tumors, and causes rapid tumor regression with a maximum of >90% remission. In the RS4;11 xenograft mouse model, BETd-260 (5 mg/kg, iv) significantly downregulates the c-Myc protein and cleaves PARP and caspase-3, breaking down the BRD2, BRD3, and BRD4 proteins for over 24 hours[1].
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| References |
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| Molecular Formula |
C43H46N10O6
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|---|---|
| Molecular Weight |
798.888748645782
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| Exact Mass |
798.36
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| Elemental Analysis |
C, 64.65; H, 5.80; N, 17.53; O, 12.02
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| CAS # |
2093388-62-4
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| PubChem CID |
131698639
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
59
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| Complexity |
1550
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UZXANFBIRSYHGO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C43H46N10O6/c1-5-53-34(20-30(50-53)25-13-14-25)46-39-37-27-19-33(58-4)28(36-22(2)51-59-23(36)3)18-31(27)45-38(37)48-40(49-39)42(56)44-17-8-6-7-10-24-11-9-12-26-29(24)21-52(43(26)57)32-15-16-35(54)47-41(32)55/h9,11-12,18-20,25,32H,5-8,10,13-17,21H2,1-4H3,(H,44,56)(H,47,54,55)(H2,45,46,48,49)
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| Chemical Name |
4-[(5-cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-[5-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]pentyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
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| Synonyms |
ZBC-260 ZBC 260 ZBC260
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). 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 : ~25 mg/mL (~31.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2517 mL | 6.2587 mL | 12.5174 mL | |
| 5 mM | 0.2503 mL | 1.2517 mL | 2.5035 mL | |
| 10 mM | 0.1252 mL | 0.6259 mL | 1.2517 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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