WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406667
CAS#: 303727-31-3
Description: L-779450 is a potent, selective and ATP-competitive Raf kinase inhibitor (IC50 = 10 nM). L-779450 suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
MedKoo Cat#: 406667
Name: L-779450
CAS#: 303727-31-3
Chemical Formula: C20H14ClN3O
Exact Mass: 347.08254
Molecular Weight: 347.8
Elemental Analysis: C, 69.07; H, 4.06; Cl, 10.19; N, 12.08; O, 4.60
Synonym: L779450; L-779450; L 779450; L779,450; L 779,450; L-779,450.
IUPAC/Chemical Name: 2-chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-imidazol-4-yl)phenol
InChi Key: WXJLXRNWMLWVFB-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H14ClN3O/c21-16-7-6-15(12-17(16)25)19-18(13-8-10-22-11-9-13)23-20(24-19)14-4-2-1-3-5-14/h1-12,25H,(H,23,24)
SMILES Code: OC1=CC(C2=C(C3=CC=NC=C3)NC(C4=CC=CC=C4)=N2)=CC=C1Cl
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
| Biological target: | L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM. |
| In vitro activity: | The pan-RAF inhibitor L-779,450 was applied for understanding the relations of RAF inhibition and apoptosis regulation in melanoma cells. Strong and dose-dependent phosphorylated ERK (pERK) downregulation was seen by L-779,450 in the BRAF(V600E)-mutated, TRAIL-sensitive melanoma cell line A-375, as well as in TRAIL-resistant A-375-TS. Reference: J Invest Dermatol. 2014 Feb;134(2):430-440. https://pubmed.ncbi.nlm.nih.gov/23955071/ |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.67 | 128.44 | |
| DMF | 30.0 | 86.26 | |
| DMF:PBS (pH 7.2) (1:7) | 0.12 | 0.35 | |
| Ethanol | 2.0 | 5.75 |
The following data is based on the product molecular weight 347.8 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 |
| Formulation protocol: | 1. Berger A, Quast SA, Plötz M, Kuhn NF, Trefzer U, Eberle J. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J Invest Dermatol. 2014 Feb;134(2):430-440. doi: 10.1038/jid.2013.347. Epub 2013 Aug 16. PMID: 23955071. |
| In vitro protocol: | 1. Berger A, Quast SA, Plötz M, Kuhn NF, Trefzer U, Eberle J. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J Invest Dermatol. 2014 Feb;134(2):430-440. doi: 10.1038/jid.2013.347. Epub 2013 Aug 16. PMID: 23955071. |
| In vivo protocol: | TBD |
1: Geserick P, Herlyn M, Leverkus M. On the TRAIL to overcome BRAF-inhibitor resistance. J Invest Dermatol. 2014 Feb;134(2):315-8. doi: 10.1038/jid.2013.348. PubMed PMID: 24424456.
2: Berger A, Quast SA, Plötz M, Kuhn NF, Trefzer U, Eberle J. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J Invest Dermatol. 2014 Feb;134(2):430-40. doi: 10.1038/jid.2013.347. Epub 2013 Aug 16. PubMed PMID: 23955071.
3: McKay MM, Ritt DA, Morrison DK. RAF inhibitor-induced KSR1/B-RAF binding and its effects on ERK cascade signaling. Curr Biol. 2011 Apr 12;21(7):563-8. doi: 10.1016/j.cub.2011.02.033. Epub 2011 Mar 31. PubMed PMID: 21458265; PubMed Central PMCID: PMC3075323.
4: Takle AK, Bamford MJ, Davies S, Davis RP, Dean DK, Gaiba A, Irving EA, King FD, Naylor A, Parr CA, Ray AM, Reith AD, Smith BB, Staton PC, Steadman JG, Stean TO, Wilson DM. The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4373-6. doi: 10.1016/j.bmcl.2008.06.070. Epub 2008 Jun 24. PubMed PMID: 18621524.
5: Shelton JG, Moye PW, Steelman LS, Blalock WL, Lee JT, Franklin RA, McMahon M, McCubrey JA. Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia. 2003 Sep;17(9):1765-82. PubMed PMID: 12970777.
