Encorafenib
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MedKoo CAT#: 205852

CAS#: 1269440-17-6

Description: Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 950 Same day
500mg USD 2130 Same day
Inquire bulk and customized quantity

Pricing updated 2020-08-03. Prices are subject to change without notice.

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


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205852
Name: Encorafenib
CAS#: 1269440-17-6
Chemical Formula: C22H27ClFN7O4S
Exact Mass: 539.15178
Molecular Weight: 540.01
Elemental Analysis: C, 48.93; H, 5.04; Cl, 6.57; F, 3.52; N, 18.16; O, 11.85; S, 5.94


Related CAS #: 1269440-17-6   1269440-29-0 (R-isomer of LGX-818)    

Synonym: LGX818; LGX-818; LGX 818; Encorafenib.

IUPAC/Chemical Name: (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate.

InChi Key: CMJCXYNUCSMDBY-ZDUSSCGKSA-N

InChi Code: InChI=1S/C22H27ClFN7O4S/c1-12(2)31-11-16(17-6-7-25-21(28-17)26-10-13(3)27-22(32)35-4)20(29-31)15-8-14(23)9-18(19(15)24)30-36(5,33)34/h6-9,11-13,30H,10H2,1-5H3,(H,27,32)(H,25,26,28)/t13-/m0/s1

SMILES Code: O=C(OC)N[C@@H](C)CNC1=NC=CC(C2=CN(C(C)C)N=C2C3=CC(Cl)=CC(NS(=O)(C)=O)=C3F)=N1


Technical Data

Appearance:
Solid powder

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

Safety Data Sheet (SDS):

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, not in water

Shelf Life:
>2 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).

HS Tariff Code:
2934.99.9001


Additional Information

  
 The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival.
 
 


References

1: Carr MJ, Sun J, Eroglu Z, Zager JS. An evaluation of encorafenib for the treatment of melanoma. Expert Opin Pharmacother. 2019 Nov 30:1-7. doi: 10.1080/14656566.2019.1694664. [Epub ahead of print] PubMed PMID: 31790307.

2: McLoughlin EM, Fadul CE, Patel SH, Hall RD, Gentzler RD. Clinical and Radiographic Response of Leptomeningeal and Brain Metastases to Encorafenib and Binimetinib in a Patient With BRAF V600E-Mutated Lung Adenocarcinoma. J Thorac Oncol. 2019 Dec;14(12):e269-e271. doi: 10.1016/j.jtho.2019.07.019. PubMed PMID: 31757377.

3: Gravbrot N, Sundararajan S. Severe Drug-Induced Liver Injury from Combination Encorafenib/Binimetinib. Case Rep Oncol Med. 2019 Oct 7;2019:3051945. doi: 10.1155/2019/3051945. eCollection 2019. PubMed PMID: 31687241; PubMed Central PMCID: PMC6800898.

4: Holbrook K, Lutzky J, Davies MA, Davis JM, Glitza IC, Amaria RN, Diab A, Patel SP, Amin A, Tawbi H. Intracranial antitumor activity with encorafenib plus binimetinib in patients with melanoma brain metastases: A case series. Cancer. 2019 Oct 28. doi: 10.1002/cncr.32547. [Epub ahead of print] PubMed PMID: 31658370.

5: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK547988/ PubMed PMID: 31643320.

6: Binimetinib plus encorafenib for metastatic melanoma. Aust Prescr. 2019 Oct;42(5):168. doi: 10.18773/austprescr.2019.057. Epub 2019 Sep 13. Review. PubMed PMID: 31631932; PubMed Central PMCID: PMC6787304.

7: Kopetz S, Grothey A, Yaeger R, Van Cutsem E, Desai J, Yoshino T, Wasan H, Ciardiello F, Loupakis F, Hong YS, Steeghs N, Guren TK, Arkenau HT, Garcia-Alfonso P, Pfeiffer P, Orlov S, Lonardi S, Elez E, Kim TW, Schellens JHM, Guo C, Krishnan A, Dekervel J, Morris V, Calvo Ferrandiz A, Tarpgaard LS, Braun M, Gollerkeri A, Keir C, Maharry K, Pickard M, Christy-Bittel J, Anderson L, Sandor V, Tabernero J. Encorafenib, Binimetinib, and Cetuximab in BRAF V600E-Mutated Colorectal Cancer. N Engl J Med. 2019 Oct 24;381(17):1632-1643. doi: 10.1056/NEJMoa1908075. Epub 2019 Sep 30. PubMed PMID: 31566309.

8: Ngo P, Bycroft R. Encorafenib and binimetinib for the treatment of BRAF-mutated metastatic melanoma in the setting of combined hepatic and renal impairment. BMJ Case Rep. 2019 Sep 16;12(9). pii: e230974. doi: 10.1136/bcr-2019-230974. PubMed PMID: 31527213.

9: Gogas HJ, Flaherty KT, Dummer R, Ascierto PA, Arance A, Mandala M, Liszkay G, Garbe C, Schadendorf D, Krajsova I, Gutzmer R, Sileni VC, Dutriaux C, de Groot JWB, Yamazaki N, Loquai C, Gollerkeri A, Pickard MD, Robert C. Adverse events associated with encorafenib plus binimetinib in the COLUMBUS study: incidence, course and management. Eur J Cancer. 2019 Sep;119:97-106. doi: 10.1016/j.ejca.2019.07.016. Epub 2019 Aug 19. PubMed PMID: 31437754.

10: Li J, Li X. Encorafenib inhibits migration, induces cell cycle arrest and apoptosis in colorectal cancer cells. Mol Cell Biochem. 2019 Sep;459(1-2):113-120. doi: 10.1007/s11010-019-03554-3. Epub 2019 May 21. PubMed PMID: 31114933.

11: Rose AAN. Encorafenib and binimetinib for the treatment of BRAF V600E/K-mutated melanoma. Drugs Today (Barc). 2019 Apr;55(4):247-264. doi: 10.1358/dot.2019.55.4.2958476. Review. PubMed PMID: 31050693.

12: Livingstone E. Evaluation of cutaneous adverse events of encorafenib and binimetinb: COMMENT on article by Graf et al. J Eur Acad Dermatol Venereol. 2019 Apr;33(4):630-631. doi: 10.1111/jdv.15527. PubMed PMID: 30924242.

13: Van Cutsem E, Huijberts S, Grothey A, Yaeger R, Cuyle PJ, Elez E, Fakih M, Montagut C, Peeters M, Yoshino T, Wasan H, Desai J, Ciardiello F, Gollerkeri A, Christy-Bittel J, Maharry K, Sandor V, Schellens JHM, Kopetz S, Tabernero J. Binimetinib, Encorafenib, and Cetuximab Triplet Therapy for Patients With BRAF V600E-Mutant Metastatic Colorectal Cancer: Safety Lead-In Results From the Phase III BEACON Colorectal Cancer Study. J Clin Oncol. 2019 Jun 10;37(17):1460-1469. doi: 10.1200/JCO.18.02459. Epub 2019 Mar 20. PubMed PMID: 30892987.

14: Brue A, Benzaquen M, Bonnet N, Koeppel MC, Default A, Delaporte E, Berbis P. Desensitization protocol for angio-oedema induced by encorafenib in a patient with metastatic melanoma. J Eur Acad Dermatol Venereol. 2019 Jul;33(7):e271-e272. doi: 10.1111/jdv.15544. Epub 2019 Mar 27. PubMed PMID: 30835914.

15: Trojaniello C, Festino L, Vanella V, Ascierto PA. Encorafenib in combination with binimetinib for unresectable or metastatic melanoma with BRAF mutations. Expert Rev Clin Pharmacol. 2019 Mar;12(3):259-266. doi: 10.1080/17512433.2019.1570847. Epub 2019 Jan 24. Review. PubMed PMID: 30652516.

16: Sun J, Zager JS, Eroglu Z. Encorafenib/binimetinib for the treatment of BRAF-mutant advanced, unresectable, or metastatic melanoma: design, development, and potential place in therapy. Onco Targets Ther. 2018 Dec 14;11:9081-9089. doi: 10.2147/OTT.S171693. eCollection 2018. Review. PubMed PMID: 30588020; PubMed Central PMCID: PMC6299465.

17: Graf NP, Koelblinger P, Galliker N, Conrad S, Barysch M, Mangana J, Dummer R, Cheng PF, Goldinger SM. The spectrum of cutaneous adverse events during encorafenib and binimetinib treatment in B-rapidly accelerated fibrosarcoma-mutated advanced melanoma. J Eur Acad Dermatol Venereol. 2019 Apr;33(4):686-692. doi: 10.1111/jdv.15363. Epub 2018 Dec 13. PubMed PMID: 30468696.

18: Dummer R, Ascierto PA, Gogas HJ, Arance A, Mandala M, Liszkay G, Garbe C, Schadendorf D, Krajsova I, Gutzmer R, Chiarion Sileni V, Dutriaux C, de Groot JWB, Yamazaki N, Loquai C, Moutouh-de Parseval LA, Pickard MD, Sandor V, Robert C, Flaherty KT. Overall survival in patients with BRAF-mutant melanoma receiving encorafenib plus binimetinib versus vemurafenib or encorafenib (COLUMBUS): a multicentre, open-label, randomised, phase 3 trial. Lancet Oncol. 2018 Oct;19(10):1315-1327. doi: 10.1016/S1470-2045(18)30497-2. Epub 2018 Sep 12. Erratum in: Lancet Oncol. 2018 Oct;19(10):e509. PubMed PMID: 30219628.

19: Martin-Liberal J. Encorafenib plus binimetinib: an embarrassment of riches. Lancet Oncol. 2018 Oct;19(10):1263-1264. doi: 10.1016/S1470-2045(18)30530-8. Epub 2018 Sep 12. PubMed PMID: 30219625.

20: Diamantopoulos PT, Stoungioti S, Anastasopoulou A, Papaxoinis G, Gogas H. Incomplete Vogt-Koyanagi-Harada disease following treatment with encorafenib and binimetinib for metastatic melanoma. Melanoma Res. 2018 Dec;28(6):648-651. doi: 10.1097/CMR.0000000000000505. PubMed PMID: 30169430.