Monometil auristatin F - Monomethyl auristatin F

Monometil auristatin F
Ismlar
	IUPAC nomi (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S) -N, 3-dimetil-2 - ((S) -3-metil-2- (metilamino) butanamido) butanamido) -3-metoksi-5-metilheptanoyl) pirrolidin-2-yl) -3-metoksi-2-metilpropanamido) -3-fenilpropanoik kislota
Identifikatorlar
CAS raqami	745017-94-1 ;
3D model (JSmol )	Interaktiv rasm;
Qisqartmalar	MMAF
ChemSpider	8570614;
PubChem CID	10395173;
UNII	1Z1AI9IW5L ;
	InChI InChI = 1S / C39H65N5O8 / c1-12-25 (6) 34 (43 (9) 38 (48) 33 (24 (4) 5) 42-37 (47) 32 (40-8) 23 (2) 3)) 30 (51-10) 22-31 (45) 44-20-16-19-29 (44) 35 (52-11) 26 (7) 36 (46) 41-28 (39 (49) 50) 21- 27-17-14-13-15-18-27 / h13-15,17-18,23-26,28-30,32-35,40H, 12,16,19-22H2,1-11H3, (H , 41,46) (H, 42,47) (H, 49,50) / t25-, 26 +, 28-, 29-, 30 +, 32-, 33-, 34-, 35 + / m0 / s1 Kalit: MFRNYXJJRJQHNW-DEMKXPNLSA-N; InChI = 1 / C39H65N5O8 / c1-12-25 (6) 34 (43 (9) 38 (48) 33 (24 (4) 5) 42-37 (47) 32 (40-8) 23 (2) 3)) 30 (51-10) 22-31 (45) 44-20-16-19-29 (44) 35 (52-11) 26 (7) 36 (46) 41-28 (39 (49) 50) 21- 27-17-14-13-15-18-27 / h13-15,17-18,23-26,28-30,32-35,40H, 12,16,19-22H2,1-11H3, (H , 41,46) (H, 42,47) (H, 49,50) / t25-, 26 +, 28-, 29-, 30 +, 32-, 33-, 34-, 35 + / m0 / s1 Kalit: MFRNYXJJRJQHNW-DEMKXPNLBL;
	Jilmayganlar O = C (N2 [C @ H] ([C @ H] (OC) [C @ H] (C (= O) N [C @ H] (C (= O) O) Cc1ccccc1) C) CCC2) " C [C @@ H] (OC) [C @@ H] (N (C (= O) [C @@ H] (NC (= O) [C @@ H] (NC) C (C) C ) C (C) C) C) [C @@ H] (C) CC;
Xususiyatlari
Kimyoviy formulalar	C39H65N5O8
Molyar massa	731.976 g · mol−1
	Boshqacha ko'rsatilmagan hollar bundan mustasno, ulardagi materiallar uchun ma'lumotlar keltirilgan standart holat (25 ° C [77 ° F], 100 kPa da).
	Infobox ma'lumotnomalari

Monometil auristatin F (MMAF) sintetik hisoblanadi antineoplastik vosita.^[1] Bu tasdiqlangan preparatning bir qismidir belantamab mafodotin yilda ko'p miyeloma va ba'zi eksperimental saratonga qarshi saraton antikor-dori konjugatlari kabi vorsetuzumab mafodotin va SGN-CD19A. Yilda Xalqaro nomuvofiq nomlar MMAF-antikor-konjugatlar uchun ism mafodotin MMAF va uning antikorga biriktirilgan tuzilishini nazarda tutadi.^[2]

Ta'sir mexanizmi

Monometil auristatin F - bu an antimitotik vosita bu inhibe qiladi hujayraning bo'linishi ning polimerizatsiyasini blokirovka qilish orqali tubulin. U saraton hujayralaridagi tuzilmalarga yuqori darajada yaqin bo'lgan antikor bilan bog'lanib, MMAFni bunday hujayralarda to'planishiga olib keladi.^[3]

Kimyo

MMAF aslida desmetil-auristatin F; ya'ni N-terminal amino guruhda faqat bittasi bor metil auristatin F ning o'zida bo'lgani kabi, o'rniga ikkita.^[3]

MMAF konjugatining tuzilishi a monoklonal antikor (MAB). Ilova guruhi quyidagilardan iborat maleimid va kapro kislotasi. Taxminan sakkizta bunday tuzilish bitta antikor molekulasi bilan bog'langan.^[3]

Shuningdek qarang

Monometil auristatin E

Adabiyotlar

^ Tai, Y. T .; Mayes, P. A .; Acharya, C; Zhong, M. Y .; Cea, M; Kagnetta, A; Kreygen, J; Yeyts, J; Gliddon, L; Fieles, Vt; Xoang, B; Tunstid, J; Kristi, A. L.; Kung, A. L .; Richardson, P; Munshi, N. C .; Anderson, K. C. (2014). "Yangi afukozillangan anti-B hujayraning kamolotga ega antigen-monometil auristatin F antikor-dori konjugati (GSK2857916) ko'p miqdordagi miyelomga qarshi kuchli va selektiv faollikni keltirib chiqaradi". Qon. 123 (20): 3128–38. doi:10.1182 / qon-2013-10-535088. PMC 4023420. PMID 24569262.
^ USAN Kengashi tomonidan qabul qilingan nomuvofiq nom to'g'risidagi bayonot: Mafodotin
^ ^a ^b ^v Dosio, F.; Brusa, P .; Kattel, L. (2011). "Immunotoksinlar va saratonga qarshi dori-darmonlarni birlashtiruvchi birikmalar: komponentlar orasidagi bog'lanishning roli". Toksinlar. 3 (12): 848–883. doi:10.3390 / toksinlar 3070848. PMC 3202854. PMID 22069744.

[1] Tai, Y. T .; Mayes, P. A .; Acharya, C; Zhong, M. Y .; Cea, M; Kagnetta, A; Kreygen, J; Yeyts, J; Gliddon, L; Fieles, Vt; Xoang, B; Tunstid, J; Kristi, A. L.; Kung, A. L .; Richardson, P; Munshi, N. C .; Anderson, K. C. (2014). "Yangi afukozillangan anti-B hujayraning kamolotga ega antigen-monometil auristatin F antikor-dori konjugati (GSK2857916) ko'p miqdordagi miyelomga qarshi kuchli va selektiv faollikni keltirib chiqaradi". Qon. 123 (20): 3128–38. doi:10.1182 / qon-2013-10-535088. PMC 4023420. PMID 24569262.

[2] USAN Kengashi tomonidan qabul qilingan nomuvofiq nom to'g'risidagi bayonot: Mafodotin

[Dosio-3] v Dosio, F.; Brusa, P .; Kattel, L. (2011). "Immunotoksinlar va saratonga qarshi dori-darmonlarni birlashtiruvchi birikmalar: komponentlar orasidagi bog'lanishning roli". Toksinlar. 3 (12): 848–883. doi:10.3390 / toksinlar 3070848. PMC 3202854. PMID 22069744.

[1]

[2]

[3]

Ismlar

IUPAC nomi (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S) -N, 3-dimetil-2 - ((S) -3-metil-2- (metilamino) butanamido) butanamido) -3-metoksi-5-metilheptanoyl) pirrolidin-2-yl) -3-metoksi-2-metilpropanamido) -3-fenilpropanoik kislota
Identifikatorlar
CAS raqami	745017-94-1^Y
3D model (JSmol )	Interaktiv rasm
Qisqartmalar	MMAF
ChemSpider	8570614
PubChem CID	10395173
UNII	1Z1AI9IW5L^Y
InChI InChI = 1S / C39H65N5O8 / c1-12-25 (6) 34 (43 (9) 38 (48) 33 (24 (4) 5) 42-37 (47) 32 (40-8) 23 (2) 3)) 30 (51-10) 22-31 (45) 44-20-16-19-29 (44) 35 (52-11) 26 (7) 36 (46) 41-28 (39 (49) 50) 21- 27-17-14-13-15-18-27 / h13-15,17-18,23-26,28-30,32-35,40H, 12,16,19-22H2,1-11H3, (H , 41,46) (H, 42,47) (H, 49,50) / t25-, 26 +, 28-, 29-, 30 +, 32-, 33-, 34-, 35 + / m0 / s1 Kalit: MFRNYXJJRJQHNW-DEMKXPNLSA-N InChI = 1 / C39H65N5O8 / c1-12-25 (6) 34 (43 (9) 38 (48) 33 (24 (4) 5) 42-37 (47) 32 (40-8) 23 (2) 3)) 30 (51-10) 22-31 (45) 44-20-16-19-29 (44) 35 (52-11) 26 (7) 36 (46) 41-28 (39 (49) 50) 21- 27-17-14-13-15-18-27 / h13-15,17-18,23-26,28-30,32-35,40H, 12,16,19-22H2,1-11H3, (H , 41,46) (H, 42,47) (H, 49,50) / t25-, 26 +, 28-, 29-, 30 +, 32-, 33-, 34-, 35 + / m0 / s1 Kalit: MFRNYXJJRJQHNW-DEMKXPNLBL
Jilmayganlar O = C (N2 [C @ H] ([C @ H] (OC) [C @ H] (C (= O) N [C @ H] (C (= O) O) Cc1ccccc1) C) CCC2) " C [C @@ H] (OC) [C @@ H] (N (C (= O) [C @@ H] (NC (= O) [C @@ H] (NC) C (C) C ) C (C) C) C) [C @@ H] (C) CC
Xususiyatlari
Kimyoviy formulalar	C₃₉H₆₅N₅O₈
Molyar massa	731.976 g · mol⁻¹
Boshqacha ko'rsatilmagan hollar bundan mustasno, ulardagi materiallar uchun ma'lumotlar keltirilgan standart holat (25 ° C [77 ° F], 100 kPa da).
Infobox ma'lumotnomalari