LC 2
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MedKoo CAT#: 465593

CAS#: 2502156-03-6

Description: LC 2 is a mutant-selective PROTAC® Degrader of KRAS, comprising a ligand for the von Hippel Lindau E3 ligase joined to the KRAS inhibitor MRTX849. LC 2 induces selective degradation of KRASG12C in cancer cell lines without inducing degradation of any other mutants (DC50 = 0.25-0.76 μM), leading to suppression of MAPK signaling and modulation of ERK signaling in both homozygous and heterozygous KRASG12C cancer cell lines. LC 2 inhibits phosphorylation of ERK in SW1573 cell lines.

Chemical Structure

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LC 2
CAS# 2502156-03-6
Instruction

Theoretical Analysis

MedKoo Cat#: 465593
Name: LC 2
CAS#: 2502156-03-6
Chemical Formula: C59H71ClFN11O7S
Exact Mass: 1,131.49
Molecular Weight: 1,132.795
Elemental Analysis: C, 62.56; H, 6.32; Cl, 3.13; F, 1.68; N, 13.60; O, 9.89; S, 2.83

Price and Availability

Size Price Availability Quantity
5mg USD 460 2 Weeks
10mg USD 850 2 Weeks
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Synonym: LC 2; LC2; LC-2;

IUPAC/Chemical Name: (2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

InChi Key: ZCGQZLKPUVGCBQ-HLMPTVQRSA-N

InChi Code: InChI=1S/C59H71ClFN11O7S/c1-37(61)56(76)71-27-26-70(32-42(71)19-22-62)54-45-20-25-69(48-14-7-11-40-10-6-13-46(60)51(40)48)34-47(45)65-58(67-54)79-35-43-12-8-23-68(43)24-9-28-78-29-21-50(74)66-53(59(3,4)5)57(77)72-33-44(73)30-49(72)55(75)63-31-39-15-17-41(18-16-39)52-38(2)64-36-80-52/h6-7,10-11,13-18,36,42-44,49,53,73H,1,8-9,12,19-21,23-35H2,2-5H3,(H,63,75)(H,66,74)/t42-,43-,44+,49-,53+/m0/s1

SMILES Code: CC1=C(SC=N1)C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCOCCCN4CCC[C@H]4COC5=NC(N6CCN([C@@H](CC#N)C6)C(C(F)=C)=O)=C7CCN(CC7=N5)C8=CC=CC9=C8C(Cl)=CC=C9)=O)C(C)(C)C)=O)=O)C=C2

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 113.3 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 1,132.80 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:
In vitro protocol:
In vivo protocol:

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1: Bond MJ, Chu L, Nalawansha DA, Li K, Crews CM. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020 Aug 26;6(8):1367-1375. doi: 10.1021/acscentsci.0c00411. Epub 2020 Jul 8. PMID: 32875077; PMCID: PMC7453568.