≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Protected from light,Argon charged,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET , with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .
In Vitro
BETd-260 (ZBC260; Compound 23) is capable of inducing degradation of BRD2, BRD3, and BRD4 proteins at 30–100 pM in the RS4;11 leukemia cells. BETd-260 shows inhibitory activity against the growth of RS4;11 leukemia cells and MOLM-13 cells with IC 50 s of 51 pM and 2.2 nM, respectively, and induces apoptosis in both RS4;11 and MOLM-13 cell lines at 3-10 nM. BETd-260 reciprocally modulates the expression of several apoptotic genes in HCC cells, i.e., suppressing the expression of anti-apoptotic Mcl-1, Bcl-2, c-Myc, and XIAP, whereas increasing the expression of pro-apoptotic Bad. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:BRD4 <30 pM (IC 50 ) BRD2 30-100 pM (IC 50 ) BRD3 30-100 pM (IC 50 )
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 분류 | Isoindoles and derivatives |
| Subclass | Isoindolines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Isoindolones |
| Alternative Parents | Alpha amino acids and derivatives Pyrrolo[2,3-d]pyrimidines Pyrimidinecarboxylic acids and derivatives Isoindoles Indoles Piperidinediones Anisoles 2-heteroaryl carboxamides Delta lactams Aminopyrimidines and derivatives Alkyl aryl ethers Imidolactams Tertiary carboxylic acid amides Pyrroles Pyrazoles N-unsubstituted carboxylic acid imides Isoxazoles Heteroaromatic compounds Dicarboximides Secondary carboxylic acid amides Secondary amines Oxacyclic compounds Azacyclic compounds Organopnictogen compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Isoindolone - Alpha-amino acid or derivatives - Pyrrolo[2,3-d]pyrimidine - Pyrrolopyrimidine - Pyrimidine-2-carboxylic acid or derivatives - Isoindole - Indole or derivatives - Indole - 2-heteroaryl carboxamide - Piperidinedione - Anisole - Piperidinone - Delta-lactam - Aminopyrimidine - Alkyl aryl ether - Imidolactam - Benzenoid - Pyrimidine - Piperidine - Heteroaromatic compound - Tertiary carboxylic acid amide - Pyrrole - Pyrazole - Carboxylic acid imide, n-unsubstituted - Isoxazole - Dicarboximide - Carboxylic acid imide - Azole - Secondary carboxylic acid amide - Lactam - Carboxamide group - Amino acid or derivatives - Oxacycle - Azacycle - Secondary amine - Ether - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Carbonyl group - Amine - Aromatic heteropolycyclic compound |
| 설명 | This compound belongs to the class of organic compounds known as isoindolones. These are aromatic polycyclic compounds that an isoindole bearing a ketone. |
| External Descriptors | Not available |
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| 용해성 | DMSO : 25 mg/mL (31.29 mM; Need ultrasonic) |
|---|---|
| 분자량 | 798.900 g/mol |
| XLogP3 | 5.300 |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 11 |
| Rotatable Bond Count | 14 |
| Exact Mass | 798.36 Da |
| Monoisotopic Mass | 798.36 Da |
| Topological Polar Surface Area | 202.000 Ų |
| Heavy Atom Count | 59 |
| Formal Charge | 0 |
| Complexity | 1550.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
