Tovorafenib | CAS#1096708-71-2 | Raf Kinase Inhibitor

MedKoo Cat#: 205777 | Name: Tovorafenib

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Tovorafenib. also known as TAK-580, MLN2480, BIIB024, and AMG 2112819, DAY101, is an oral, selective pan-Raf kinase inhibitor. The Raf kinases (A-Raf, B-Raf and C-Raf) are key regulators of cell proliferation and survival within the mitogen-activated protein kinase (MAPK) pathway. The MAPK pathway is frequently disregulated in human cancers, often via activating mutations of Ras or Raf.

Chemical Structure

Tovorafenib

CAS#1096708-71-2

Theoretical Analysis

MedKoo Cat#: 205777

Name: Tovorafenib

CAS#: 1096708-71-2

Chemical Formula: C17H12Cl2F3N7O2S

Exact Mass: 505.0102

Molecular Weight: 506.29

Elemental Analysis: C, 40.33; H, 2.39; Cl, 14.01; F, 11.26; N, 19.37; O, 6.32; S, 6.33

Price and Availability

Size	Price	Availability
5mg	USD 250.00	2 Weeks
1g	USD 4,650.00	3 months
2g	USD 7,950.00	3 months

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Related CAS #

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Synonym

AMG 2112819; AMG2112819; AMG2112819; BIIB 024; BIIB 024; BIIB024; BUB 024; BUB024; BUB-024; MLN 2480; MLN2480; MLN-2480; TAK 580; TAK580; TAK-580; DAY101; DAY-101; DAY 101;Tovorafenib;

IUPAC/Chemical Name

(R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide

InChi Key

VWMJHAFYPMOMGF-ZCFIWIBFSA-N

InChi Code

InChI=1S/C17H12Cl2F3N7O2S/c1-6(28-15(31)12-11(19)13(23)27-5-26-12)16-25-4-9(32-16)14(30)29-10-2-7(17(20,21)22)8(18)3-24-10/h2-6H,1H3,(H,28,31)(H2,23,26,27)(H,24,29,30)/t6-/m1/s1

SMILES Code

O=C(C1=CN=C([C@H](NC(C2=NC=NC(N)=C2Cl)=O)C)S1)NC3=NC=C(Cl)C(C(F)(F)F)=C3

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, 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

More Info

Instruction

View handling instruction

	Solvent	mg/mL	mM
Solubility
	DMSO	20.0	39.50
	Ethanol	20.0	39.50

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 506.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Tkacik E, Li K, Gonzalez-Del Pino G, Ha BH, Vinals J, Park E, Beyett TS, Eck MJ. Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib. J Biol Chem. 2023 May;299(5):104634. doi: 10.1016/j.jbc.2023.104634. Epub 2023 Mar 22. PMID: 36963492; PMCID: PMC10149214. 2: Rasco DW, Medina T, Corrie P, Pavlick AC, Middleton MR, Lorigan P, Hebert C, Plummer R, Larkin J, Agarwala SS, Daud AI, Qiu J, Bozon V, Kneissl M, Barry E, Olszanski AJ. Phase 1 study of the pan-RAF inhibitor tovorafenib in patients with advanced solid tumors followed by dose expansion in patients with metastatic melanoma. Cancer Chemother Pharmacol. 2023 Jul;92(1):15-28. doi: 10.1007/s00280-023-04544-5. Epub 2023 May 23. PMID: 37219686; PMCID: PMC10261210. 3: Targeted Options for Glioma Looking Good. Cancer Discov. 2023 Aug 4;13(8):1755. doi: 10.1158/2159-8290.CD-ND2023-0004. PMID: 37276325. 4: Offer K, McGuire MT, Song K, Goldfischer MJ, Davare MA, Corless CL, Beadling C, Neff T, Cox MC, Govinda Raju S, Blackman SC. Activity of Type II RAF Inhibitor Tovorafenib in a Pediatric Patient With a Recurrent Spindle Cell Sarcoma Harboring a Novel SNX8-BRAF Gene Fusion. JCO Precis Oncol. 2023 Jul;7:e2300065. doi: 10.1200/PO.23.00065. PMID: 37410972; PMCID: PMC10581647. 5: Kilburn LB, Khuong-Quang DA, Hansford JR, Landi D, van der Lugt J, Leary SES, Driever PH, Bailey S, Perreault S, McCowage G, Waanders AJ, Ziegler DS, Witt O, Baxter PA, Kang HJ, Hassall TE, Han JW, Hargrave D, Franson AT, Yalon Oren M, Toledano H, Larouche V, Kline C, Abdelbaki MS, Jabado N, Gottardo NG, Gerber NU, Whipple NS, Segal D, Chi SN, Oren L, Tan EEK, Mueller S, Cornelio I, McLeod L, Zhao X, Walter A, Da Costa D, Manley P, Blackman SC, Packer RJ, Nysom K. The type II RAF inhibitor tovorafenib in relapsed/refractory pediatric low-grade glioma: the phase 2 FIREFLY-1 trial. Nat Med. 2024 Jan;30(1):207-217. doi: 10.1038/s41591-023-02668-y. Epub 2023 Nov 17. Erratum in: Nat Med. 2024 May;30(5):1500. doi: 10.1038/s41591-024-02910-1. PMID: 37978284; PMCID: PMC10803270. 6: Sidaway P. Tovorafenib effective against low-grade gliomas harbouring BRAF fusions. Nat Rev Clin Oncol. 2024 Feb;21(2):83. doi: 10.1038/s41571-023-00845-z. PMID: 38082106. 7: van Tilburg CM, Kilburn LB, Perreault S, Schmidt R, Azizi AA, Cruz-Martínez O, Zápotocký M, Scheinemann K, Meeteren AYNS, Sehested A, Opocher E, Driever PH, Avula S, Ziegler DS, Capper D, Koch A, Sahm F, Qiu J, Tsao LP, Blackman SC, Manley P, Milde T, Witt R, Jones DTW, Hargrave D, Witt O. LOGGIC/FIREFLY-2: a phase 3, randomized trial of tovorafenib vs. chemotherapy in pediatric and young adult patients with newly diagnosed low-grade glioma harboring an activating RAF alteration. BMC Cancer. 2024 Jan 30;24(1):147. doi: 10.1186/s12885-024-11820-x. PMID: 38291372; PMCID: PMC10826080. 8: Yaman I, Bouffet E. How will tovorafenib change our treatment of pediatric low-grade glioma? Expert Opin Emerg Drugs. 2024 Mar;29(1):1-3. doi: 10.1080/14728214.2024.2312817. Epub 2024 Feb 2. PMID: 38293894. 9: Kilburn LB, Khuong-Quang DA, Hansford JR, Landi D, van der Lugt J, Leary SES, Driever PH, Bailey S, Perreault S, McCowage G, Waanders AJ, Ziegler DS, Witt O, Baxter PA, Kang HJ, Hassall TE, Han JW, Hargrave D, Franson AT, Yalon Oren M, Toledano H, Larouche V, Kline C, Abdelbaki MS, Jabado N, Gottardo NG, Gerber NU, Whipple NS, Segal D, Chi SN, Oren L, Tan EEK, Mueller S, Cornelio I, McLeod L, Zhao X, Walter A, Da Costa D, Manley P, Blackman SC, Packer RJ, Nysom K. Author Correction: The type II RAF inhibitor tovorafenib in relapsed/refractory pediatric low-grade glioma: the phase 2 FIREFLY-1 trial. Nat Med. 2024 May;30(5):1500. doi: 10.1038/s41591-024-02910-1. Erratum for: Nat Med. 2024 Jan;30(1):207-217. doi: 10.1038/s41591-023-02668-y. PMID: 38467878; PMCID: PMC11108768. 10: Khoury JE, Wehbe S, Attieh F, Boutros M, Kesrouani C, Kourie HR. A critical review of RAF inhibitors in BRAF-mutated glioma treatment. Pharmacogenomics. 2024;25(7):343-355. doi: 10.1080/14622416.2024.2355859. Epub 2024 Jun 3. PMID: 38884947; PMCID: PMC11404696. 11: Tovorafenib (Ojemda) for pediatric low-grade glioma. Med Lett Drugs Ther. 2024 Jun 10;66(1704):e97-e98. doi: 10.58347/tml.2024.1704f. PMID: 38905536. 12: Dhillon S. Tovorafenib: First Approval. Drugs. 2024 Aug;84(8):985-993. doi: 10.1007/s40265-024-02069-6. Epub 2024 Jul 5. PMID: 38967715. 13: Zhang T, Xu B, Tang F, He Z, Zhou J. Type II RAF inhibitor tovorafenib for the treatment of pediatric low-grade glioma. Expert Rev Clin Pharmacol. 2024 Oct 19:1-10. doi: 10.1080/17512433.2024.2418405. Epub ahead of print. PMID: 39412085.