Pexidartinib HCl
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MedKoo CAT#: 207104

CAS#: 2040295-03-0 (HCl)

Description: Pexidartinib, also know as PLX-3397, is a CSF1R inhibitor with IC50 of 20 nM in development by Plexxikon for the treatment of tenosynovial giant cell tumors. It is in a phase 3 clinical trial for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS).


Price and Availability

Size
Price

100mg
USD 150
1g
USD 750
10g
USD 3850
Size
Price

200mg
USD 250
2g
USD 1250
20g
USD 6850
Size
Price

500mg
USD 450
5g
USD 2650

Pexidartinib HCl, purity > 98%, is in stock. The same day shipping after order received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 207104
Name: Pexidartinib HCl
CAS#: 2040295-03-0 (HCl)
Chemical Formula: C20H16Cl2F3N5
Exact Mass:
Molecular Weight: 454.2782
Elemental Analysis: C, 52.88; H, 3.55; Cl, 15.61; F, 12.55; N, 15.42


Related CAS #: 1029044-16-3 (free base)   2040295-03-0 (HCl)   2169310-71-6 (2HCl)    

Synonym: PLX3397; PLX-3397; PLX 3397; CML-261; CML 261; CML261; FP-113; FP 113; FP113; Pexidartinib HCl; Pexidartinib hydrochloride; Turalio;

IUPAC/Chemical Name: 5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine hydrochloride

InChi Key: CJLUYLRKLUYCEK-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H15ClF3N5.ClH/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24;/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29);1H

SMILES Code: FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F.[H]Cl


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934.99.90.01


References

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2: Lamb YN. Pexidartinib: First Approval. Drugs. 2019 Nov;79(16):1805-1812. doi: 10.1007/s40265-019-01210-0. Review. PubMed PMID: 31602563.

3: Mason C, Kossatz S, Carter L, Pirovano G, Brand C, Guru N, Pérez-Medina C, Lewis JS, Mulder W, Reiner T. A (89)Zr-HDL PET tracer monitors response to a CSF1R inhibitor. J Nucl Med. 2019 Aug 16. pii: jnumed.119.230466. doi: 10.2967/jnumed.119.230466. [Epub ahead of print] PubMed PMID: 31420495.

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11: Merry TL, Brooks AES, Masson SW, Adams SE, Jaiswal JK, Jamieson SMF, Shepherd PR. The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Int J Obes (Lond). 2019 Mar 29. doi: 10.1038/s41366-019-0355-7. [Epub ahead of print] PubMed PMID: 30926949.

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14: Lee JH, Chen TW, Hsu CH, Yen YH, Yang JC, Cheng AL, Sasaki SI, Chiu LL, Sugihara M, Ishizuka T, Oguma T, Tajima N, Lin CC. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors. Invest New Drugs. 2019 Mar 2. doi: 10.1007/s10637-019-00745-z. [Epub ahead of print] PubMed PMID: 30825104.

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16: Qiao S, Qian Y, Xu G, Luo Q, Zhang Z. Long-term characterization of activated microglia/macrophages facilitating the development of experimental brain metastasis through intravital microscopic imaging. J Neuroinflammation. 2019 Jan 7;16(1):4. doi: 10.1186/s12974-018-1389-9. PubMed PMID: 30616691; PubMed Central PMCID: PMC6323850.

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20: Takeda A, Shinozaki Y, Kashiwagi K, Ohno N, Eto K, Wake H, Nabekura J, Koizumi S. Microglia mediate non-cell-autonomous cell death of retinal ganglion cells. Glia. 2018 Nov;66(11):2366-2384. doi: 10.1002/glia.23475. Epub 2018 Oct 29. PubMed PMID: 30375063.