[D-Arg1,D-Phe5,D-Trp7,9,Leu11]Substance P (trifluoroacetate salt)

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]Substance P (SPD-D) is an analog of substance P (Cay-24035) and a broad-spectrum neuropeptide antagonist with anticancer activity. It blocks intracellular calcium increases induced by vasopressin, bradykinin (Cay-37408), gastrin (Cay-24457), and galanin (Cay-24456) in H-510 small cell lung carcinoma (SCLC) cells. SPD-D also blocks vasopressin- and bradykinin-induced MAPK signaling in H-510 SCLC cells in a concentration-dependent manner. It inhibits DNA synthesis in a panel of cancer cell lines (IC50s = 20-50 µM) and reduces colony formation of HC12, ICR-SC112, HX149, and NCI-H226 cancer cells in vitro (IC50s = 0.5-6.5 µM). In vivo, SPD-D (2.1 µg, s.c.) inhibits tumor growth in HC12 and ICR-SC112 SCLC mouse xenograft models.Formal Name: D-arginyl-L-prolyl-L-lysyl-L-prolyl-D-phenylalanyl-L-glutaminyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-L-leucyl-L-leucinamide, trifluoroacetate salt. Synonyms: D-Phe5SP, L-756,867, SPD-D. Molecular Formula: C79H109N19O12 . XCF3COOH. Formula Weight: 1516.8. Purity: >95%. Formulation: (Request formulation change), A lyophilized powder. Solubility: Water: 1 mg/ml. SMILES: O=C(N[C@@H](CCCCN)C(N1CCC[C@H]1C(N[C@H](CC2=CC=CC=C2)C(N[C@@H](CCC(N)=O)C(N[C@H](CC3=CNC4=C3C=CC=C4)C(N[C@H](C(N[C@H](CC5=CNC6=C5C=CC=C6)C(N[C@H](C(N[C@H](C(N)=O)CC(C)C)=O)CC(C)C)=O)=O)CC7=CC=CC=C7)=O)=O)=O)=O)=O)[C@H]8N(C([C@H](N)CCCNC(N)=N)=O)CCC8.FC(F)(C(O)=O)F. InChi Code: InChI=1S/C79H109N19O12.C2HF3O2/c1-46(2)38-59(68(83)100)91-70(102)60(39-47(3)4)92-73(105)64(43-51-45-88-56-28-14-12-25-53(51)56)95-72(104)61(40-48-20-7-5-8-21-48)93-74(106)63(42-50-44-87-55-27-13-11-24-52(50)55)94-69(101)57(32-33-67(82)99)89-71(103)62(41-49-22-9-6-10-23-49)96-76(108)66-31-19-37-98(66)78(110)58(29-15-16-34-80)90-75(107)65-30-18-36-97(65)77(109)54(81)26-17-35-86-79(84)85,3-2(4,5)1(6)7/h5-14,20-25,27-28,44-47,54,57-66,87-88H,15-19,26,29-43,80-81H2,1-4H3,(H2,82,99)(H2,83,100)(H,89,103)(H,90,107)(H,91,102)(H,92,105)(H,93,106)(H,94,101)(H,95,104)(H,96,108)(H4,84,85,86),(H,6,7)/t54-,57+,58+,59+,60+,61+,62-,63-,64-,65+,66+,/m1./s1. InChi Key: LDPZJUMVCRKMNL-YJEREJMLSA-N.