PROTAC KRASG12C Degrader-LC-2

Product Name: PROTAC KRASG12C Degrader-LC-2
CAS No.: 2502156-03-6
Chemical Name: PROTAC KRASG12C Degrader-LC-2
Synonyms: LC-2;LC-2 ，S6996;PROTAC KRASG12C Degrader-LC-2;(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-m;(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;L-Prolinamide, N-[3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl]oxy]methyl]-1-pyrrolidinyl]propoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-
CBNumber: CB78200421
Molecular Formula: C59H71ClFN11O7S
Formula Weight: 1132.78
MOL File: 2502156-03-6.mol

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PROTAC KRASG12C Degrader-LC-2 Property

Density: 1.297±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 50 mg/mL (44.14 mM; ultrasonic and warming and heat to 80°C)
form: Solid
pka: 14.07±0.40(Predicted)
color: Off-white to brown

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0139674
Product name: LC-2
Packaging: 1mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-0139674
Product name: LC-2
Packaging: 5mg
Price: $1500
Updated: 2021/12/16

ChemScene

Product number: CS-0139674
Product name: LC-2
Packaging: 10mg
Price: $2500
Updated: 2021/12/16

ChemScene

Product number: CS-0139674
Product name: LC-2
Packaging: 25mg
Price: $4800
Updated: 2021/12/16

CSNpharm

Product number: CSN27182
Product name: LC-2
Packaging: 1mg
Price: $360
Updated: 2021/12/16

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PROTAC KRASG12C Degrader-LC-2 Chemical Properties,Usage,Production

Description

LC-2 is a von Hippel-Lindau-based PROTAC which can degrade endogenous KRAS G12C. It covalently binds KRAS G12C with a MARTX849 warhead and recruits the E3 ligase VHL which degrades the KRAS G12C and suppresses MAPK signaling in homozygous and heterzygous KRAS G12C cell lines.

Uses

LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM[1]. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines[2].

IC 50

KRAS(G12C): 0.25-0.76 μM (DC₅₀); VHL

storage

Store at -20°C

References

[1] De Vita E, et al. The Missing Link between (Un)druggable and Degradable KRAS. ACS Cent Sci. 2020;6(8):1281-1284. DOI:10.1021/acscentsci.0c00920
[2] Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375. DOI:10.1021/acscentsci.0c00411

PROTAC KRASG12C Degrader-LC-2 Preparation Products And Raw materials

Raw materials

Preparation Products

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PROTAC KRASG12C Degrader-LC-2 Suppliers

China 38 United States 2 Global 40

Bide Pharmatech Ltd.

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PROTAC KRASG12C Degrader-LC-2

LC-2

(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

(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-m

L-Prolinamide, N-[3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl]oxy]methyl]-1-pyrrolidinyl]propoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

LC-2 ，S6996

2502156-03-6