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MedKoo Cat#: 563900 | Name: Darovasertib HCl

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 HCl
Darovasertib HCl
CAS#Darovasertib HCl

Theoretical Analysis

MedKoo Cat#: 563900

Name: Darovasertib HCl

CAS#: Darovasertib HCl

Chemical Formula: C22H25Cl2F3N8O

Exact Mass: 472.1947

Molecular Weight: 544.15

Elemental Analysis: C, 48.45; H, 4.62; Cl, 13.00; F, 10.45; N, 20.55; O, 2.93

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1874276-76-2 (free base) Darovasertib HCl
Synonym
NVP-LXS196; NVPLXS196; NVP LXS196; LXS196; LXS-196; LXS 196; 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 dihydrochloride
InChi Key
HEACNZAVEISRMY-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H23F3N8O.2ClH/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);2*1H
SMILES Code
O=C(NC1=NC=CC=C1N2CCC(N)(CC2)C)C3=NC(C4=NC=CC=C4C(F)(F)F)=CN=C3N.[H]Cl.[H]Cl
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).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 544.15 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.

Recalculate based on batch purity %
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.