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Pexidartinib

Names

[ CAS No. ]:
1029044-16-3

[ Name ]:
Pexidartinib

[Synonym ]:
PLX3397
5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-{[6-(trifluoromethyl)-3-pyridinyl]methyl}-2-pyridinamine
3-Pyridinemethanamine, N-[5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-
N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine
PLX-3397
pexidartinib

Biological Activity

[Description]:

Pexidartinib (PLX-3397) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13 nM, 27 nM, and 11 nM for CSF1R, c-Kit, and FLT3, respectively.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Research Areas >> Cancer

[Target]

IC50: 28 nM (c-Fms), 16 nM (c-Kit)


[In Vivo]

Pexidartinib is a potent drug for treatment of cancer and used for Phase III TGCT clinical trial[1].

[References]

[1]. Gelhorn HL, et al. Patient-reported Symptoms of Tenosynovial Giant Cell Tumors. Clin Ther. 2016 Apr;38(4):778-93.


[Related Small Molecules]

BLZ945 | Masitinib (AB1010) | SU14813 | GW2580 | Dovitinib (TKI-258, CHIR-258) | Sitravatinib (MGCD516) | DCC-2618 | BLU-285 | Motesanib | OSI-930 | AST 487 | Ki20227 | DCC-2618 | Telatinib | Amuvatinib (MP-470)

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
580.0±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C20H15ClF3N5

[ Molecular Weight ]:
417.815

[ Flash Point ]:
304.6±30.1 °C

[ Exact Mass ]:
417.096802

[ PSA ]:
66.49000

[ LogP ]:
4.77

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.662

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds