ALRN-6924

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MedKoo CAT#: 465668

CAS#: 1451199-80-6

Description: Sulanemadlin, also known as ALRN-6924 is a novel dual MDM4 and MDM2 inhibitor. ALRN-6924 is a "stapled peptide" that mimics the N-terminal domain of the p53 tumor suppressor protein. It binds with high affinity to both MDM2 and MDMX (also known as MDM4), the endogenous inhibitors of p53, to activate p53 signaling in cells having a non-mutant, or wild-type TP53 genotype (TP53-WT). Iterative structure-activity optimization endowed ALRN-6924 with favorable cell permeability, solubility, and pharmacokinetic and safety profiles. Intracellular proteolysis of ALRN-6924 forms a long-acting active metabolite with potent MDM2 and MDMX binding affinity and slow dissociation kinetics. At high doses, ALRN-6924 exhibits on-mechanism anticancer activity in TP53-WT tumor models. At lower doses, ALRN-6924 transiently arrests the cell cycle in healthy tissues to protect them from chemotherapy without protecting the TP53-mutant cancer cells.

Chemical Structure

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ALRN-6924
CAS# 1451199-80-6
Instruction

Theoretical Analysis

MedKoo Cat#: 465668
Name: ALRN-6924
CAS#: 1451199-80-6
Chemical Formula: C93H138N20O21
Exact Mass: 1,871.03
Molecular Weight: 1,872.246
Elemental Analysis: C, 59.66; H, 7.43; N, 14.96; O, 17.95

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1451199-80-6   2000293-14-9    

Synonym: ALRN-6924; ALRN6924; ALRN 6924; Sulanemadlin;

IUPAC/Chemical Name: (2S,5S,8S,11S,14S,17S,20S,32R,E)-8-((1H-indol-3-yl)methyl)-32-((R)-2-((2S,3R)-2-((R)-2-acetamido-4-methylpentanamido)-3-hydroxybutanamido)-3-phenylpropanamido)-N-((2R,5S,8S,11S,14S,17S)-1-amino-2,5,8,11,14-pentamethyl-1,4,7,10,13,16-hexaoxo-3,6,9,12,15-pentaazaoctadecan-17-yl)-14-(3-amino-3-oxopropyl)-5-(4-hydroxybenzyl)-17-isobutyl-2,11,20,32-tetramethyl-3,6,9,12,15,18,33-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotritriacont-24-ene-20-carboxamide

InChi Key: MEGJEIYKXGSAPA-LWFCIRQHSA-N

InChi Code: InChI=1S/C93H138N20O21/c1-49(2)43-68(105-60(14)115)86(129)111-74(59(13)114)89(132)110-71(45-61-31-25-24-26-32-61)88(131)113-93(16)42-30-23-21-19-17-18-20-22-29-41-92(15,90(133)103-57(11)80(123)101-55(9)79(122)100-54(8)78(121)99-53(7)77(120)98-52(6)76(119)97-51(5)75(95)118)112-87(130)69(44-50(3)4)108-83(126)67(39-40-73(94)117)106-81(124)56(10)102-84(127)72(47-63-48-96-66-34-28-27-33-65(63)66)109-85(128)70(46-62-35-37-64(116)38-36-62)107-82(125)58(12)104-91(93)134/h18,20,24-28,31-38,48-59,67-72,74,96,114,116H,17,19,21-23,29-30,39-47H2,1-16H3,(H2,94,117)(H2,95,118)(H,97,119)(H,98,120)(H,99,121)(H,100,122)(H,101,123)(H,102,127)(H,103,133)(H,104,134)(H,105,115)(H,106,124)(H,107,125)(H,108,126)(H,109,128)(H,110,132)(H,111,129)(H,112,130)(H,113,131)/b20-18+/t51-,52+,53+,54+,55+,56+,57+,58+,59-,67+,68-,69+,70+,71-,72+,74+,92+,93-/m1/s1

SMILES Code: O=C([C@@](CCC/C=C/CCCCCC[C@]1(NC([C@H](NC([C@@H](NC([C@H](NC(C)=O)CC(C)C)=O)[C@H](O)C)=O)CC2=CC=CC=C2)=O)C)(C)NC([C@H](CC(C)C)NC([C@H](CCC(N)=O)NC([C@H](C)NC([C@H](CC3=CNC4=C3C=CC=C4)NC([C@H](CC5=CC=C(O)C=C5)NC([C@H](C)NC1=O)=O)=O)=O)=O)=O)=O)N[C@@H](C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@H](C)C(N)=O)=O)=O)=O)=O)=O

Appearance: 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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,872.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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