L-779450
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    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.

Chemical Structure

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L-779450
CAS# 303727-31-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406667
Name: L-779450
CAS#: 303727-31-3
Chemical Formula: C20H14ClN3O
Exact Mass: 347.08
Molecular Weight: 347.800
Elemental Analysis: C, 69.07; H, 4.06; Cl, 10.19; N, 12.08; O, 4.60

Price and Availability

Size Price Availability Quantity
10mg USD 90 Ready to ship
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 750 Ready to ship
500mg USD 1350 Ready to ship
1g USD 2250 2 Weeks
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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

More Info:         

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.7 128.44
DMF 30.0 86.26
DMF:PBS (pH 7.2) (1:7) 0.1 0.35
Ethanol 2.0 5.75

Preparing Stock Solutions

The following data is based on the product molecular weight 347.80 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
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

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 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.