Darovasertib free base | CAS#1874276-76-2

MedKoo Cat#: 206824 | Name: Darovasertib free base

Featured

Description:

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

Darovasertib, also known as LXS-196 and NVP-LXS196, is a potent and orally active protein kinase C inhibitor for the treatment of uveal melanoma. Upon oral administration, protein kinase C inhibitor LXS196 binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival.

Chemical Structure

Darovasertib free base

CAS#1874276-76-2 (free base)

Theoretical Analysis

MedKoo Cat#: 206824

Name: Darovasertib free base

CAS#: 1874276-76-2 (free base)

Chemical Formula: C22H23F3N8O

Exact Mass: 472.1947

Molecular Weight: 472.48

Elemental Analysis: C, 55.93; H, 4.91; F, 12.06; N, 23.72; O, 3.39

Price and Availability

Size	Price	Availability
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,450.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 4,850.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

1874276-76-2 (free base) Darovasertib HCl

Synonym

NVP-LXS196; NVPLXS196; NVP LXS196; LXS-196; LXS 196; LXS196; LXS-196 free base; Darovasertib;

IUPAC/Chemical Name

3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide

InChi Key

XXJXHXJWQSCNPX-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H23F3N8O/c1-21(27)6-10-33(11-7-21)15-5-3-9-29-19(15)32-20(34)17-18(26)30-12-14(31-17)16-13(22(23,24)25)4-2-8-28-16/h2-5,8-9,12H,6-7,10-11,27H2,1H3,(H2,26,30)(H,29,32,34)

SMILES Code

NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1

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

>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

Preparing Stock Solutions

The following data is based on the product molecular weight 472.48 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: Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG. Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma. J Med Chem. 2024 Jan 25;67(2):1447-1459. doi: 10.1021/acs.jmedchem.3c02002. Epub 2024 Jan 10. PMID: 38198520. 2: Arang N, Lubrano S, Ceribelli M, Rigiracciolo DC, Saddawi-Konefka R, Faraji F, Ramirez SI, Kim D, Tosto FA, Stevenson E, Zhou Y, Wang Z, Bogomolovas J, Molinolo AA, Swaney DL, Krogan NJ, Yang J, Coma S, Pachter JA, Aplin AE, Alessi DR, Thomas CJ, Gutkind JS. High-throughput chemogenetic drug screening reveals PKC-RhoA/PKN as a targetable signaling vulnerability in GNAQ-driven uveal melanoma. Cell Rep Med. 2023 Nov 21;4(11):101244. doi: 10.1016/j.xcrm.2023.101244. Epub 2023 Oct 18. PMID: 37858338; PMCID: PMC10694608. 3: Hiong A, O'Day R, Fog LS, McKay D, McKenzie J, Ameratunga M, Joshua AM, Shackleton M. Globe Salvage and Vision Preservation by Neoadjuvant Darovasertib and Crizotinib in Uveal Melanoma. Ophthalmol Retina. 2023 Oct 17:S2468-6530(23)00501-8. doi: 10.1016/j.oret.2023.10.009. Epub ahead of print. PMID: 37852320. 4: Cao L, Chen S, Sun R, Ashby CR Jr, Wei L, Huang Z, Chen ZS. Darovasertib, a novel treatment for metastatic uveal melanoma. Front Pharmacol. 2023 Jul 28;14:1232787. doi: 10.3389/fphar.2023.1232787. PMID: 37576814; PMCID: PMC10419210. 5: Rodrigues A, Cosman R, Joshua AM. LXS196 for Metastatic Uveal Melanoma - finally some progress. Br J Cancer. 2023 May;128(10):1791-1793. doi: 10.1038/s41416-023-02199-w. Epub 2023 Mar 1. Erratum in: Br J Cancer. 2023 Mar 28;: PMID: 36859685; PMCID: PMC10147608. 6: Malik AU, Karapetsas A, Nirujogi RS, Chatterjee D, Phung TK, Wightman M, Gourlay R, Morrice N, Mathea S, Knapp S, Alessi DR. PKC isoforms activate LRRK1 kinase by phosphorylating conserved residues (Ser1064, Ser1074 and Thr1075) within the CORB GTPase domain. Biochem J. 2022 Sep 30;479(18):1941-1965. doi: 10.1042/BCJ20220308. PMID: 36040231; PMCID: PMC9555798. 7: Shoushtari AN, Khan S, Komatsubara K, Feun L, Acquavella N, Singh-Kandah S, Negri T, Nesson A, Abbate K, Cremers S, Musi E, Ambrosini G, Lee S, Schwartz GK, Carvajal RD. A Phase Ib Study of Sotrastaurin, a PKC Inhibitor, and Alpelisib, a PI3Kα Inhibitor, in Patients with Metastatic Uveal Melanoma. Cancers (Basel). 2021 Nov 2;13(21):5504. doi: 10.3390/cancers13215504. PMID: 34771668; PMCID: PMC8583628.

View History

Ethionine