NMR, HPLC, LCMS, COA, Pls kindly check:
Name: Cobimetinib
CAS: 934660-93-2
Chemical Formula: C22H22F3IN2O2
Exact Mass: 530.06781
Molecular Weight: 530.32196
Elemental Analysis: C, 49.83; H, 4.18; F, 10.75; I, 23.93; N, 5.28; O, 6.03
Related CAS #: 1369665-02-0 (fumarate) 934660-93-2 (free base)
Synonym: XL518; XL 518; XL-518; GDC0973; GDC 0973; GDC-0973; cobimetinib.
TECHNICAL DATA
Appearance: white 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).
REFERENCES
1: Choo EF, Ng CM, Berry L, Belvin M, Lewin-Koh N, Merchant M, Salphati L. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. doi: 10.1007/s00280-012-1988-6. Epub 2012 Oct 7. PubMed PMID: 23053270.
2: Baudy AR, Dogan T, Flores-Mercado JE, Hoeflich KP, Su F, van Bruggen N, Williams SP. FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973. EJNMMI Res. 2012 May 31;2(1):22. doi: 10.1186/2191-219X-2-22. PubMed PMID: 22651703; PubMed Central PMCID: PMC3405466.
3: Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L, Engst S, Joshi AA, Kennedy AR, Kim AI, Koltun ES, Lougheed JC, Manalo JC, Martini JF, Nuss JM, Peto CJ, Tsang TH, Yu P, Johnston S. Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med Chem Lett. 2012 Apr 9;3(5):416-21. doi: 10.1021/ml300049d. eCollection 2012 May 10. PubMed PMID: 24900486; PubMed Central PMCID: PMC4025802.
4: Wong H, Vernillet L, Peterson A, Ware JA, Lee L, Martini JF, Yu P, Li C, Del Rosario G, Choo EF, Hoeflich KP, Shi Y, Aftab BT, Aoyama R, Lam ST, Belvin M, Prescott J. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. doi: 10.1158/1078-0432.CCR-12-0445. Epub 2012 Apr 10. PubMed PMID: 22496205.
5: Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH. Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions. Drug Metab Dispos.
CAS: 934660-93-2
Chemical Formula: C22H22F3IN2O2
Exact Mass: 530.06781
Molecular Weight: 530.32196
Elemental Analysis: C, 49.83; H, 4.18; F, 10.75; I, 23.93; N, 5.28; O, 6.03
Related CAS #: 1369665-02-0 (fumarate) 934660-93-2 (free base)
Synonym: XL518; XL 518; XL-518; GDC0973; GDC 0973; GDC-0973; cobimetinib.
TECHNICAL DATA
Appearance: white 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).
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1: Choo EF, Ng CM, Berry L, Belvin M, Lewin-Koh N, Merchant M, Salphati L. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. doi: 10.1007/s00280-012-1988-6. Epub 2012 Oct 7. PubMed PMID: 23053270.
2: Baudy AR, Dogan T, Flores-Mercado JE, Hoeflich KP, Su F, van Bruggen N, Williams SP. FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973. EJNMMI Res. 2012 May 31;2(1):22. doi: 10.1186/2191-219X-2-22. PubMed PMID: 22651703; PubMed Central PMCID: PMC3405466.
3: Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L, Engst S, Joshi AA, Kennedy AR, Kim AI, Koltun ES, Lougheed JC, Manalo JC, Martini JF, Nuss JM, Peto CJ, Tsang TH, Yu P, Johnston S. Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med Chem Lett. 2012 Apr 9;3(5):416-21. doi: 10.1021/ml300049d. eCollection 2012 May 10. PubMed PMID: 24900486; PubMed Central PMCID: PMC4025802.
4: Wong H, Vernillet L, Peterson A, Ware JA, Lee L, Martini JF, Yu P, Li C, Del Rosario G, Choo EF, Hoeflich KP, Shi Y, Aftab BT, Aoyama R, Lam ST, Belvin M, Prescott J. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. doi: 10.1158/1078-0432.CCR-12-0445. Epub 2012 Apr 10. PubMed PMID: 22496205.
5: Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH. Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions. Drug Metab Dispos.
