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. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is 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; Pexidartinib; Pexidartinib HCl; Pexidartinib hydrochloride

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)

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

1: Wesolowski R, Sharma N, Reebel L, Rodal MB, Peck A, West BL, Marimuthu A, Severson P, Karlin DA, Dowlati A, Le MH, Coussens LM, Rugo HS. Phase Ib study of the combination of pexidartinib (PLX3397), a CSF-1R inhibitor, and paclitaxel in patients with advanced solid tumors. Ther Adv Med Oncol. 2019 Jun 21;11:1758835919854238. doi: 10.1177/1758835919854238. eCollection 2019. PubMed PMID: 31258629; PubMed Central PMCID: PMC6589951.

2: Piawah S, Hyland C, Umetsu SE, Esserman LJ, Rugo HS, Chien AJ. A case report of vanishing bile duct syndrome after exposure to pexidartinib (PLX3397) and paclitaxel. NPJ Breast Cancer. 2019 Jun 14;5:17. doi: 10.1038/s41523-019-0112-z. eCollection 2019. PubMed PMID: 31240240; PubMed Central PMCID: PMC6570645.

3: Tap WD, Gelderblom H, Palmerini E, Desai J, Bauer S, Blay JY, Alcindor T, Ganjoo K, Martín-Broto J, Ryan CW, Thomas DM, Peterfy C, Healey JH, van de Sande M, Gelhorn HL, Shuster DE, Wang Q, Yver A, Hsu HH, Lin PS, Tong-Starksen S, Stacchiotti S, Wagner AJ; ENLIVEN investigators. Pexidartinib versus placebo for advanced tenosynovial giant cell tumour (ENLIVEN): a randomised phase 3 trial. Lancet. 2019 Jun 19. pii: S0140-6736(19)30764-0. doi: 10.1016/S0140-6736(19)30764-0. [Epub ahead of print] PubMed PMID: 31229240.

4: Rosenbaum E, Kelly C, D'Angelo SP, Dickson MA, Gounder M, Keohan ML, Movva S, Condy M, Adamson T, Mcfadyen CR, Antonescu CR, Hwang S, Singer S, Qin LX, Tap WD, Chi P. A Phase I Study of Binimetinib (MEK162) Combined with Pexidartinib (PLX3397) in Patients with Advanced Gastrointestinal Stromal Tumor. Oncologist. 2019 Jun 18. pii: theoncologist.2019-0418. doi: 10.1634/theoncologist.2019-0418. [Epub ahead of print] PubMed PMID: 31213500.

5: Li X, Jue L, Wang S, Pang X. [Pexidartinib inhibits the aggregation of monocytes into tumor microenvironment and reduces the number of M2 tumor-associated macrophages]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2019 Apr;35(4):307-312. Chinese. PubMed PMID: 31167689.

6: Miladinovic T, Sharma M, Phan A, Geres H, Ungard RG, Linher-Melville K, Singh G. Activation of hippocampal microglia in a murine model of cancer-induced pain. J Pain Res. 2019 Mar 18;12:1003-1016. doi: 10.2147/JPR.S191860. eCollection 2019. PubMed PMID: 30936739; PubMed Central PMCID: PMC6430067.

7: 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.

8: 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.

9: Yao J, Du Z, Li Z, Zhang S, Lin Y, Li H, Zhou L, Wang Y, Yan G, Wu X, Duan Y, Du G. 6-Gingerol as an arginase inhibitor prevents urethane-induced lung carcinogenesis by reprogramming tumor supporting M2 macrophages to M1 phenotype. Food Funct. 2018 Sep 19;9(9):4611-4620. doi: 10.1039/c8fo01147h. PubMed PMID: 30151521.

10: Kuse Y, Ohuchi K, Nakamura S, Hara H, Shimazawa M. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018. PubMed PMID: 30090016; PubMed Central PMCID: PMC6066272.

11: Giustini N, Bernthal NM, Bukata SV, Singh AS. Tenosynovial giant cell tumor: case report of a patient effectively treated with pexidartinib (PLX3397) and review of the literature. Clin Sarcoma Res. 2018 Jul 10;8:14. doi: 10.1186/s13569-018-0101-2. eCollection 2018. PubMed PMID: 30002809; PubMed Central PMCID: PMC6038319.

12: Dammeijer F, Lievense LA, Kaijen-Lambers ME, van Nimwegen M, Bezemer K, Hegmans JP, van Hall T, Hendriks RW, Aerts JG. Depletion of Tumor-Associated Macrophages with a CSF-1R Kinase Inhibitor Enhances Antitumor Immunity and Survival Induced by DC Immunotherapy. Cancer Immunol Res. 2017 Jul;5(7):535-546. doi: 10.1158/2326-6066.CIR-16-0309. Epub 2017 May 23. PubMed PMID: 28536100.

13: Gelhorn HL, Tong S, McQuarrie K, Vernon C, Hanlon J, Maclaine G, Lenderking W, Ye X, Speck RM, Lackman RD, Bukata SV, Healey JH, Keedy VL, Anthony SP, Wagner AJ, Von Hoff DD, Singh AS, Becerra CR, Hsu HH, Lin PS, Tap WD. Patient-reported Symptoms of Tenosynovial Giant Cell Tumors. Clin Ther. 2016 Apr;38(4):778-93. doi: 10.1016/j.clinthera.2016.03.008. Epub 2016 Apr 1. PubMed PMID: 27041409; PubMed Central PMCID: PMC5469507.