For research use only. Not for therapeutic Use.
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research[1].
Sulanemadlin (0-10 μM, 24 h) induces reversible, dose-dependent cell cycle arrest in CD34+ human bone marrow cells, and protects cells from Topotecan (HY-13768)-induced DNA damage[2].
Sulanemadlin (5-20 mg/kg, i.v.) shows antitumor activity in multiple TP53-WT subcutaneous mouse xenograft models[1].
Sulanemadlin (2.4 mg/kg, daily with for 5 days, 24 h prior to daily 1.5 mg/kg Topotecan) protects mice against Topotecan-induced neutropenia and gastrointestinal toxicity in mice, without diminishing Topotecan antitumor activity in TP53-mutant cancer models[1].
PK properties of Sulanemadlin.
Species
Dose (mg/kg)
Cmax (μg/mL)
AUCall (μg·h/mL)
T1/2 (h)
CL (mL/h/kg)
Mouse
5
67.8
450
2.2
11
Rat
5
95.9
223
2.0
24
Monkey
5
137
914
4.9
5.9
| Catalog Number | I041621 |
| CAS Number | 1451199-98-6 |
| Synonyms | 3-[(2S,5S,8S,11S,14S,17S,20S,24E,32R)-32-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-20-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-amino-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-14-(3-amino-3-oxopropyl)-5-[(4-hydroxyphenyl)methyl]-8-(1H-indol-3-ylmethyl)-11,20,32-trimethyl-17-(2-methylpropyl)-3,6,9,12,15,18,33-heptaoxo-1,4,7,10,13,16,19-heptazacyclotritriacont-24-en-2-yl]propanoic acid |
| Molecular Formula | C95H140N20O23 |
| Purity | ≥95% |
| InChI | InChI=1S/C95H140N20O23/c1-50(2)44-69(106-60(13)117)88(133)113-76(59(12)116)91(136)111-72(46-61-30-24-23-25-31-61)90(135)115-95(15)43-29-22-20-18-16-17-19-21-28-42-94(14,92(137)105-58(11)82(127)103-56(9)81(126)102-55(8)80(125)101-54(7)79(124)100-53(6)78(123)99-52(5)77(97)122)114-89(134)70(45-51(3)4)108-84(129)67(38-40-74(96)119)107-83(128)57(10)104-86(131)73(48-63-49-98-66-33-27-26-32-65(63)66)110-87(132)71(47-62-34-36-64(118)37-35-62)109-85(130)68(112-93(95)138)39-41-75(120)121/h17,19,23-27,30-37,49-59,67-73,76,98,116,118H,16,18,20-22,28-29,38-48H2,1-15H3,(H2,96,119)(H2,97,122)(H,99,123)(H,100,124)(H,101,125)(H,102,126)(H,103,127)(H,104,131)(H,105,137)(H,106,117)(H,107,128)(H,108,129)(H,109,130)(H,110,132)(H,111,136)(H,112,138)(H,113,133)(H,114,134)(H,115,135)(H,120,121)/b19-17+/t52-,53+,54+,55+,56+,57+,58+,59-,67+,68+,69+,70+,71+,72+,73+,76+,94+,95-/m1/s1 |
| InChIKey | VDLGAZDAHPLOIR-RLPDZDIMSA-N |
| SMILES | CC1C(=O)NC(C(=O)NC(C(=O)NC(CCCC=CCCCCCCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)CCC(=O)O)(C)NC(=O)C(CC5=CC=CC=C5)NC(=O)C(C(C)O)NC(=O)C(CC(C)C)NC(=O)C)(C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C)C(=O)N)CC(C)C)CCC(=O)N |
| Reference | [1]. Manuel AIVADO, et al. Peptidomimetic macrocycles and uses thereof. WO2018208954A2 |
