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MedKoo Cat#: 465561 | Name: CG 858
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CG 858 is a selective BRAF-V600E protein Degrader (uSMITETM). CG 858 comprises the BRAF kinase inhibitor vemurafenib linked to the E3 ligase ligand Thalidomide. CG 858 dose-dependently degrades BRAF-V600E but not wild type BRAF, and reduces cell viability and colony formation in HT-29 and A375 cells (DC50 values are 124 nM and 500 nM, respectively). It exhibits 88% degradation at 500 nM. CG 858 also impairs melanoma cell growth.

Chemical Structure

CG 858
CG 858
CAS#2417296-82-1

Theoretical Analysis

MedKoo Cat#: 465561

Name: CG 858

CAS#: 2417296-82-1

Chemical Formula: C42H39F2N7O8S

Exact Mass: 839.2549

Molecular Weight: 839.87

Elemental Analysis: C, 60.06; H, 4.68; F, 4.52; N, 11.67; O, 15.24; S, 3.82

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
CG 858; CG858; CG-858;
IUPAC/Chemical Name
N-(4-(3-(2,6-difluoro-3-(propylsulfonamido)benzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)-5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)pentanamide
InChi Key
AAIPPJPUZKZIHC-UHFFFAOYSA-N
InChi Code
InChI=1S/C42H39F2N7O8S/c1-2-17-60(58,59)50-32-13-12-31(43)36(37(32)44)38(54)30-22-48-39-28(30)18-25(21-47-39)24-8-6-23(7-9-24)20-46-34(52)5-3-4-16-45-26-10-11-27-29(19-26)42(57)51(41(27)56)33-14-15-35(53)49-40(33)55/h6-13,18-19,21-22,33,45,50H,2-5,14-17,20H2,1H3,(H,46,52)(H,47,48)(H,49,53,55)
SMILES Code
CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(C=C23)C4=CC=C(CNC(CCCCNC5=CC=C6C(N(C7CCC(NC7=O)=O)C(C6=C5)=O)=O)=O)C=C4)=O)=C1F)=O
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
Solvent mg/mL mM comments
Solubility
DMSO 84.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 839.87 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: Hameleers A, Most J, Schotanus M, Wijnands N, Dremmen M, van Vugt R, Boonen B. Return to work after proximal humeral fractures: a single center study comparing conservative versus operative treatment. Orthop Rev (Pavia). 2025 Jan 27;17:128106. doi: 10.52965/001c.128106. PMID: 39882031; PMCID: PMC11779521. 2: Yang Y, Guo W, Sun J, Chen Q, Meng X, Wang L, Tao H, Yang L. Characteristics of volatile organic compounds and secondary organic aerosol pollution in different functional areas of petrochemical industrial cities in Northwest China. Sci Total Environ. 2023 Feb 1;858(Pt 3):159903. doi: 10.1016/j.scitotenv.2022.159903. Epub 2022 Nov 2. PMID: 36334656. 3: Tian H, Xu W, Wen L, Tang L, Zhang X, Song T, Yang C. Association of TLR3 gene 1377C/T (rs3775290) and TLR7 gene C/G (rs3853839) polymorphism with hand, foot, and mouth disease caused by human enterovirus 71 infection susceptibility and severity in the Chinese Han population: A meta-analysis of case-control studies. Medicine (Baltimore). 2022 Jul 8;101(27):e29758. doi: 10.1097/MD.0000000000029758. PMID: 35801751; PMCID: PMC9259132. 4: Capasso M, Ciuca L, Procesi IG, Zinno F, Berrilli F, Cringoli G, Rinaldi L. Single and Synergistic Effects of Fenbendazole and Metronidazole Against Subclinical Infection by Giardia duodenalis in Non-Human Primates in a Zoological Garden in Southern Italy. Front Vet Sci. 2022 Jun 16;9:929443. doi: 10.3389/fvets.2022.929443. PMID: 35782538; PMCID: PMC9244615. 5: Campbell AS, Ho CCG, Atık M, Allen M, Lincoln S, Malphrus K, Nguyen T, Oatman SR, Corda M, Conway O, Strickland S, Petersen RC, Dickson DW, Graff-Radford NR, Ertekin-Taner N. Clinical Deep Phenotyping of ABCA7 Mutation Carriers. Neurol Genet. 2022 Jan 13;8(2):e655. doi: 10.1212/NXG.0000000000000655. PMID: 35047668; PMCID: PMC8759075. 6: Shafiei F, Dehghanian P, Ghaderi N, Doozandeh M. Fracture resistance of endodontically treated premolars restored with bulk-fill composite resins: The effect of fiber reinforcement. Dent Res J (Isfahan). 2021 Jul 19;18:60. PMID: 34497695; PMCID: PMC8404566. 7: Tjokrowidjaja A, Friedlander M, Lord SJ, Asher R, Rodrigues M, Ledermann JA, Matulonis UA, Oza AM, Bruchim I, Huzarski T, Gourley C, Harter P, Vergote I, Scott CL, Meier W, Shapira-Frommer R, Milenkova T, Pujade-Lauraine E, Gebski V, Lee CK. Prognostic nomogram for progression-free survival in patients with BRCA mutations and platinum-sensitive recurrent ovarian cancer on maintenance olaparib therapy following response to chemotherapy. Eur J Cancer. 2021 Sep;154:190-200. doi: 10.1016/j.ejca.2021.06.024. Epub 2021 Jul 19. PMID: 34293664. 8: Liu WX, Yang L, Yan HM, Yan LN, Zhang XL, Ma N, Tang LM, Gao X, Liu DW. Germline Variants and Genetic Interactions of Several EMT Regulatory Genes Increase the Risk of HBV-Related Hepatocellular Carcinoma. Front Oncol. 2021 Jun 11;11:564477. doi: 10.3389/fonc.2021.564477. PMID: 34178612; PMCID: PMC8226114. 9: Ameri B, Mohammadi Zardkhoshoui A, Hosseiny Davarani SS. Metal-organic- framework derived hollow manganese nickel selenide spheres confined with nanosheets on nickel foam for hybrid supercapacitors. Dalton Trans. 2021 Jun 22;50(24):8372-8384. doi: 10.1039/d1dt01215k. PMID: 34037022. 10: Oh J, Pradella D, Shao C, Li H, Choi N, Ha J, Ruggiero S, Fu XD, Zheng X, Ghigna C, Shen H. Widespread Alternative Splicing Changes in Metastatic Breast Cancer Cells. Cells. 2021 Apr 9;10(4):858. doi: 10.3390/cells10040858. PMID: 33918758; PMCID: PMC8070448. 11: Xu K, An N, Huang H, Duan L, Ma J, Ding J, He T, Zhu J, Li Z, Cheng X, Zhou G, Ba Y. Fluoride exposure and intelligence in school-age children: evidence from different windows of exposure susceptibility. BMC Public Health. 2020 Nov 4;20(1):1657. doi: 10.1186/s12889-020-09765-4. Retraction in: BMC Public Health. 2022 Nov 8;22(1):2044. doi: 10.1186/s12889-022-14470-5. PMID: 33148225; PMCID: PMC7640398. 12: Nai YH, Teo BW, Tan NL, Chua KYW, Wong CK, O'Doherty S, Stephenson MC, Schaefferkoetter J, Thian YL, Chiong E, Reilhac A. Evaluation of Multimodal Algorithms for the Segmentation of Multiparametric MRI Prostate Images. Comput Math Methods Med. 2020 Oct 20;2020:8861035. doi: 10.1155/2020/8861035. PMID: 33144873; PMCID: PMC7596462. 13: Fujiwara T, Kobayashi T, Yasuma T, D'Alessandro-Gabazza CN, Toda M, Fujimoto H, Fujiwara K, Takeshita A, Nishihama K, Okano T, D'Alessandro VF, Takei Y, Hataji O, Gabazza EC. De Novo T790M Mutation in an L858R Epidermal Growth Factor Receptor Mutant-Associated Lung Adenocarcinoma. Cancers (Basel). 2020 Oct 21;12(10):3074. doi: 10.3390/cancers12103074. PMID: 33096790; PMCID: PMC7589092. 14: Zhang Y, Zhou YM, Zhang ZJ, Li X. miR-210 is a Serological Biomarker for Predicting Recurrence and Prognosis of Colon Carcinoma Patients with Liver Metastases After Radiofrequency Ablation Treatment. Cancer Manag Res. 2020 Sep 25;12:9077-9085. doi: 10.2147/CMAR.S267731. PMID: 33061602; PMCID: PMC7524199. 15: Wan S, Zhao H. Analysis of diagnostic and prognostic value of lncRNA MEG3 in cervical cancer. Oncol Lett. 2020 Nov;20(5):183. doi: 10.3892/ol.2020.12044. Epub 2020 Aug 31. PMID: 32934750; PMCID: PMC7471741. 16: Zhang Y, Liu C, Cheng H, Tian S, Liu Y, Wang S, Zhang H, Saqib M, Wei H, Wei Z. DNA methylation and its effects on gene expression during primary to secondary growth in poplar stems. BMC Genomics. 2020 Jul 20;21(1):498. doi: 10.1186/s12864-020-06902-6. PMID: 32689934; PMCID: PMC7372836. 17: Wood R, Liu AG, Bowyer F, Wilby PR, Dunn FS, Kenchington CG, Cuthill JFH, Mitchell EG, Penny A. Author Correction: Integrated records of environmental change and evolution challenge the Cambrian Explosion. Nat Ecol Evol. 2019 May;3(5):858. doi: 10.1038/s41559-019-0897-z. Erratum for: Nat Ecol Evol. 2019 Apr;3(4):528-538. doi: 10.1038/s41559-019-0821-6. PMID: 30979959. 18: van de Loo AJAE, van Schrojenstein Lantman M, Mackus M, Scholey A, Verster JC. Impact of mental resilience and perceived immune functioning on the severity of alcohol hangover. BMC Res Notes. 2018 Jul 31;11(1):526. doi: 10.1186/s13104-018-3659-0. PMID: 30064526; PMCID: PMC6069540. 19: Burlew CC, Sumislawski JJ, Behnfield CD, McNutt MK, McCarthy J, Sharpe JP, Croce MA, Bala M, Kashuk J, Spalding MC, Beery PR, John S, Hunt DJ, Harmon L, Stein DM, Callcut R, Wybourn C, Sperry J, Anto V, Dunn J, Veith JP, Brown CVR, Celii A, Zander TL, Coimbra R, Berndtson AE, Moss TZ, Malhotra AK, Hazelton JP, Linden K, West M, Alam HB, Williams AM, Kim J, Inaba K, Moulton S, Choi YM, Warren HL, Collier B, Ball CG, Savage S, Hartwell JL, Cullinane DC, Zielinski MD, Ray-Zack MD, Morse BC, Rhee P, Rutherford EJ, Udekwu P, Reynolds C, Toschlog E, Gondek S, Ju T, Haan JM, Lightwine KL, Kulvatunyou N, Coates B, Khouqeer AF, Todd SR, Zarzaur B, Waller CJ, Kallies KJ, Neideen T, Eddine SBZ, Peck KA, Dunne CE, Kramer K, Bokhari F, Dhillon TS, Galante JM, Cohen MJ. Time to stroke: A Western Trauma Association multicenter study of blunt cerebrovascular injuries. J Trauma Acute Care Surg. 2018 Nov;85(5):858-866. doi: 10.1097/TA.0000000000001989. PMID: 29847537. 20: Scrutinio D, Lanzillo B, Guida P, Mastropasqua F, Monitillo V, Pusineri M, Formica R, Russo G, Guarnaschelli C, Ferretti C, Calabrese G. Development and Validation of a Predictive Model for Functional Outcome After Stroke Rehabilitation: The Maugeri Model. Stroke. 2017 Dec;48(12):3308-3315. doi: 10.1161/STROKEAHA.117.018058. Epub 2017 Oct 19. PMID: 29051222.

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