Trametinib DMSO solvate
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MedKoo CAT#: 123211

CAS#: 1187431-43-1

Description: Trametinib DMSO solvate is a solvated form of trametinib at 1:1 molar ratio of trametinib to dimethyl sulfoxide. Trametinib, also known as GSK1120212, GSK212 or JTP74057, is an approved and new targeted drug for the treatment of melanoma. It is a powerful and selective MEK1/MEK2 inhibitor which can effectively prevent cancer cell proliferating and can induce cell apoptosis, and increase the life of patients.


Price and Availability

Size
Price

10mg
USD 50
1g
USD 750
Size
Price

100mg
USD 150
10g
USD 2950
Size
Price

500mg
USD 450
50g
USD 6950

Trametinib DMSO solvate, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international). Note: the estimated shipping out time for order > 5g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 123211
Name: Trametinib DMSO solvate
CAS#: 1187431-43-1
Chemical Formula: C28H29FIN5O5S
Exact Mass:
Molecular Weight: 693.09
Elemental Analysis: C, 48.49; H, 4.21; F, 2.74; I, 18.30; N, 10.10; O, 11.53; S, 4.62


Synonym: Trametinib DMSO solvate, GSK-1120212 DMSO solvate;Trametinib;JTP-74057; JTP 74057; JTP74057; GSK-1120212;GSK1120212;GSK 1120212.

IUPAC/Chemical Name: N-(3-(3-cyclopropyl-5-((2-fluoro-4-iodophenyl)amino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl)phenyl)acetamide compound with (methylsulfinyl)methane (1:1)

InChi Key: OQUFJVRYDFIQBW-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H23FIN5O4.C2H6OS/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34;1-4(2)3/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34);1-2H3

SMILES Code: CC1=C2C(C(N(C3CC3)C(N2C4=CC(NC(C)=O)=CC=C4)=O)=O)=C(NC5=C(F)C=C(I)C=C5)N(C)C1=O.CS(C)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
293490


References

1: Kasuga A, Nakagawa K, Nagashima F, Shimizu T, Naruge D, Nishina S, Kitamura H, Kurata T, Takasu A, Fujisaka Y, Okamoto W, Nishimura Y, Mukaiyama A, Matsushita H, Furuse J. A phase I/Ib study of trametinib (GSK1120212) alone and in combination with gemcitabine in Japanese patients with advanced solid tumors. Invest New Drugs. 2015 Aug 12. [Epub ahead of print] PubMed PMID: 26259955.

2: Giurcaneanu C, Nitipir C, Popa LG, Forsea AM, Popescu I, Bumbacea RS. Evolution of Melanocytic Nevi under Vemurafenib, Followed by Combination Therapy with Dabrafenib and Trametinib for Metastatic Melanoma. Acta Dermatovenerol Croat. 2015 Jul;23(2):87-95. Review. PubMed PMID: 26228819.

3: Modak S, Asante-Korang A, Steinherz LJ, Grana N. Trametinib-induced Left Ventricular Dysfunction in a Child With Relapsed Neuroblastoma. J Pediatr Hematol Oncol. 2015 Aug;37(6):e381-3. doi: 10.1097/MPH.0000000000000364. PubMed PMID: 26181424.

4: Schick U, Kyula J, Barker H, Patel R, Zaidi S, Gregory C, Hafsi H, Roulstone V, Deutsch E, McLaughlin M, Harrington K. Trametinib radiosensitises RAS- and BRAF-mutated melanoma by perturbing cell cycle and inducing senescence. Radiother Oncol. 2015 Jul 8. pii: S0167-8140(15)00323-0. doi: 10.1016/j.radonc.2015.06.026. [Epub ahead of print] PubMed PMID: 26163092.

5: Chopra N, Nathan PD. Trametinib in metastatic melanoma. Expert Rev Anticancer Ther. 2015;15(7):749-60. doi: 10.1586/14737140.2015.1060127. PubMed PMID: 26107021.

6: Melanoma: Dabrafenib and trametinib improve overall survival. Nat Rev Clin Oncol. 2015 Sep;12(9):502. doi: 10.1038/nrclinonc.2015.114. Epub 2015 Jun 23. PubMed PMID: 26099986.

7: Draganova D, Kerger J, Caspers L, Willermain F. Severe bilateral panuveitis during melanoma treatment by Dabrafenib and Trametinib. J Ophthalmic Inflamm Infect. 2015 Jun 9;5:17. doi: 10.1186/s12348-015-0049-9. eCollection 2015. PubMed PMID: 26078801; PubMed Central PMCID: PMC4460117.

8: Menzies AM, Yeh I, Botton T, Bastian BC, Scolyer RA, Long GV. Clinical activity of the MEK inhibitor trametinib in metastatic melanoma containing BRAF kinase fusion. Pigment Cell Melanoma Res. 2015 Sep;28(5):607-10. doi: 10.1111/pcmr.12388. Epub 2015 Jul 3. PubMed PMID: 26072686; PubMed Central PMCID: PMC4539279.

9: Long GV, Stroyakovskiy D, Gogas H, Levchenko E, de Braud F, Larkin J, Garbe C, Jouary T, Hauschild A, Grob JJ, Chiarion-Sileni V, Lebbe C, Mandalà M, Millward M, Arance A, Bondarenko I, Haanen JB, Hansson J, Utikal J, Ferraresi V, Kovalenko N, Mohr P, Probachai V, Schadendorf D, Nathan P, Robert C, Ribas A, DeMarini DJ, Irani JG, Swann S, Legos JJ, Jin F, Mookerjee B, Flaherty K. Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial. Lancet. 2015 Aug 1;386(9992):444-51. doi: 10.1016/S0140-6736(15)60898-4. Epub 2015 May 31. PubMed PMID: 26037941.

10: Minor DR, Puzanov I, Callahan MK, Hug BA, Hoos A. Severe gastrointestinal toxicity with administration of trametinib in combination with dabrafenib and ipilimumab. Pigment Cell Melanoma Res. 2015 Sep;28(5):611-2. doi: 10.1111/pcmr.12383. Epub 2015 Jun 23. PubMed PMID: 25996827.

11: Escandell I, Cabezas M, Martín JM, Terradez L, Pinazo MI. Effective treatment with Dabrafenib and Trametinib for a BRAF-mutated metastatic dedifferentiated malignant spindle cell neoplasm. J Eur Acad Dermatol Venereol. 2015 Apr 27. doi: 10.1111/jdv.13155. [Epub ahead of print] PubMed PMID: 25917403.

12: Qiu JG, Zhang YJ, Li Y, Zhao JM, Zhang WJ, Jiang QW, Mei XL, Xue YQ, Qin WM, Yang Y, Zheng DW, Chen Y, Wei MN, Shi Z. Trametinib modulates cancer multidrug resistance by targeting ABCB1 transporter. Oncotarget. 2015 Jun 20;6(17):15494-509. PubMed PMID: 25915534.

13: Fujishita T, Kajino-Sakamoto R, Kojima Y, Taketo MM, Aoki M. Antitumor activity of the MEK inhibitor trametinib on intestinal polyp formation in Apc(Δ716) mice involves stromal COX-2. Cancer Sci. 2015 Jun;106(6):692-9. doi: 10.1111/cas.12670. Epub 2015 May 1. PubMed PMID: 25855137.

14: Rissmann R, Hessel MH, Cohen AF. Vemurafenib/dabrafenib and trametinib. Br J Clin Pharmacol. 2015 Apr 6. doi: 10.1111/bcp.12651. [Epub ahead of print] PubMed PMID: 25847075.

15: Thota R, Johnson DB, Sosman JA. Trametinib in the treatment of melanoma. Expert Opin Biol Ther. 2015 May;15(5):735-47. doi: 10.1517/14712598.2015.1026323. Epub 2015 Mar 26. PubMed PMID: 25812921.

16: Schadendorf D, Amonkar MM, Stroyakovskiy D, Levchenko E, Gogas H, de Braud F, Grob JJ, Bondarenko I, Garbe C, Lebbe C, Larkin J, Chiarion-Sileni V, Millward M, Arance A, Mandalà M, Flaherty KT, Nathan P, Ribas A, Robert C, Casey M, DeMarini DJ, Irani JG, Aktan G, Long GV. Health-related quality of life impact in a randomised phase III study of the combination of dabrafenib and trametinib versus dabrafenib monotherapy in patients with BRAF V600 metastatic melanoma. Eur J Cancer. 2015 May;51(7):833-40. doi: 10.1016/j.ejca.2015.03.004. Epub 2015 Mar 17. PubMed PMID: 25794603.

17: Blumenschein GR Jr, Smit EF, Planchard D, Kim DW, Cadranel J, De Pas T, Dunphy F, Udud K, Ahn MJ, Hanna NH, Kim JH, Mazieres J, Kim SW, Baas P, Rappold E, Redhu S, Puski A, Wu FS, Jänne PA. A randomized phase II study of the MEK1/MEK2 inhibitor trametinib (GSK1120212) compared with docetaxel in KRAS-mutant advanced non-small-cell lung cancer (NSCLC)†. Ann Oncol. 2015 May;26(5):894-901. doi: 10.1093/annonc/mdv072. Epub 2015 Feb 26. PubMed PMID: 25722381.

18: Joshi M, Rice SJ, Liu X, Miller B, Belani CP. Trametinib with or without vemurafenib in BRAF mutated non-small cell lung cancer. PLoS One. 2015 Feb 23;10(2):e0118210. doi: 10.1371/journal.pone.0118210. eCollection 2015. PubMed PMID: 25706985; PubMed Central PMCID: PMC4338247.

19: Du SL, Yuan X, Zhan S, Tang LJ, Tong CY. Trametinib, a novel MEK kinase inhibitor, suppresses lipopolysaccharide-induced tumor necrosis factor (TNF)-α production and endotoxin shock. Biochem Biophys Res Commun. 2015 Mar 13;458(3):667-73. doi: 10.1016/j.bbrc.2015.01.160. Epub 2015 Feb 13. PubMed PMID: 25684183.

20: Mas C, Boda B, CaulFuty M, Huang S, Wiszniewski L, Constant S. Antitumour efficacy of the selumetinib and trametinib MEK inhibitors in a combined human airway-tumour-stroma lung cancer model. J Biotechnol. 2015 Jul 10;205:111-9. doi: 10.1016/j.jbiotec.2015.01.012. Epub 2015 Jan 20. PubMed PMID: 25615947.