BO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.

Targets

FGFR3 ; TACC3 (Cell-free assay); TACC3 (Cell-free assay) ; 1.5 nM(Kd); 188 nM

In vitro

BO-264 significantly decreases centrosomal TACC3 during both mitosis and interphase. BO-264 displays potent anti-proliferative activity in the NCI- 60 cell line panel compromising nine different cancer types. BO-264 significantly inhibits the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies.

In vivo

BO-264\'s oral administration significantly impairs tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increases survival without any major toxicity.

Cell Research(from reference)

Cell lines：JIMT-1 cells

Concentrations：1 μM

Incubation Time：6 h

사양

사양 및 순도

≥99%

생화학 및 생리적 메커니즘

BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

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순수함

≥99%

제품 특성

ALogP

3.02

hba_count

HBD 수

회전 가능한 결합

이름과 식별자

Pubchem Sid

504773613

Pubchem Sid Url

https://pubchem.ncbi.nlm.nih.gov/substance/504773613

정식 스마일

COC1=CC=C(C=C1)C2=NOC(=C2)NC3=NC(=NC=C3)N4CCOCC4

IUPAC Name

3-(4-methoxyphenyl)-N-(2-morpholin-4-ylpyrimidin-4-yl)-1,2-oxazol-5-amine

InChIKey

WRCGBYNVBFVRTN-UHFFFAOYSA-N

INCHI

1S/C18H19N5O3/c1-24-14-4-2-13(3-5-14)15-12-17(26-22-15)20-16-6-7-19-18(21-16)23-8-10-25-11-9-23/h2-7,12H,8-11H2,1H3,(H,19,20,21)

이성체 SMILES

COC1=CC=C(C=C1)C2=NOC(=C2)NC3=NC(=NC=C3)N4CCOCC4

분자량

353.38

Reaxy-Rn

35592964

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35592964&ln=

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고급 데이터

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Benzenoids
  - 분류 Phenol ethers
    - Subclass Anisoles

Kingdom	Organic compounds
Superclass	Benzenoids
분류	Phenol ethers
Subclass	Anisoles
Intermediate Tree Nodes	Not available
Direct Parent	Anisoles
Alternative Parents	Phenoxy compounds Methoxybenzenes Dialkylarylamines Aminopyrimidines and derivatives Alkyl aryl ethers Morpholines Imidolactams Isoxazoles Heteroaromatic compounds Secondary amines Oxacyclic compounds Dialkyl ethers Azacyclic compounds Organopnictogen compounds Hydrocarbon derivatives
Molecular Framework	Aromatic heteromonocyclic compounds
Substituents	Phenoxy compound - Methoxybenzene - Dialkylarylamine - Tertiary aliphatic/aromatic amine - Anisole - Aminopyrimidine - Alkyl aryl ether - Imidolactam - Pyrimidine - Oxazinane - Morpholine - Monocyclic benzene moiety - Heteroaromatic compound - Isoxazole - Azole - Tertiary amine - Oxacycle - Azacycle - Organoheterocyclic compound - Secondary amine - Ether - Dialkyl ether - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Amine - Aromatic heteromonocyclic compound
설명	This compound belongs to the class of organic compounds known as anisoles. These are organic compounds containing a methoxybenzene or a derivative thereof.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

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리뷰

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Lot Number	Certificate Type	날짜	항목
F2229150	Certificate of Analysis	Apr 03, 2025	B414300
F2229179	Certificate of Analysis	Apr 03, 2025	B414300
F2229180	Certificate of Analysis	Apr 03, 2025	B414300

용해성	Solubility (25°C) In vitro DMSO: 71 mg/mL (200.91 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg/mL) 최대 용해도	71
DMSO(mM) 최대 용해도	200.916860037354
물(mg/mL) 최대 용해도	＜1
분자량	353.400 g/mol
XLogP3	2.600
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	5
Exact Mass	353.149 Da
Monoisotopic Mass	353.149 Da
Topological Polar Surface Area	85.500 Å²
Heavy Atom Count	26
Formal Charge	0
Complexity	429.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

BO-264 - ≥99% , CAS No.2408648-20-2

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