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BO-264 - 10mM in DMSO, high purity , CAS No.2408648-20-2

    Grade & Purity:
  • 10mM in DMSO
In stock
Item Number
B422802
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B422802-1ml
1ml
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$152.90

TACC3 Inhibitors

Basic Description

Specifications & Purity 10mM in DMSO
Biochemical and Physiological Mechanisms 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
Storage Temp Store at -80°C
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Product Description

Information

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 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class 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
Description 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

Product Properties

ALogP 3.02
hba_count 6
HBD Count 1
Rotatable Bond 5

Associated Targets(Human)

CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BT-474 (2113 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MCF-12A (112 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RT-112 (346 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RT-4 (268 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCT-116 (91556 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MDA-MB-231 (73002 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAL-51 (262 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCC1143 (70 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCC1954 (381 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MDA-MB-157 (173 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JIMT-1 (237 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

EMT6 (738 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
4T1 (1737 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CT26 (928 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 3-(4-methoxyphenyl)-N-(2-morpholin-4-ylpyrimidin-4-yl)-1,2-oxazol-5-amine
INCHI 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)
InChIKey WRCGBYNVBFVRTN-UHFFFAOYSA-N
Smiles COC1=CC=C(C=C1)C2=NOC(=C2)NC3=NC(=NC=C3)N4CCOCC4
Isomeric SMILES COC1=CC=C(C=C1)C2=NOC(=C2)NC3=NC(=NC=C3)N4CCOCC4
Molecular Weight 353.38
Reaxy-Rn 35592964
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35592964&ln=

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 71
DMSO(mM) Max Solubility 200.916860037354
Water(mg / mL) Max Solubility <1
Molecular Weight 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 Ų
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

Solution Calculators

Reviews

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