| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
CST626 targets inhibitor of apoptosis proteins (IAPs). It is a pan-IAP degrader that degrades XIAP, cIAP1, and cIAP2 in MM.1S cells, with DC50 values of 0.7 nM, 2.4 nM, and 6.2 nM, respectively. It also shows activity against other IAP family members.
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| ln Vitro |
Compound 9, or CST626; its DC50 values are 2.4 nM, 6.2 nM, and 0.7 nM, respectively, and they cause the degradation of cIAP1, cIAP2, and XIAP in a dose-dependent manner [1]. The vitality of cancer cells is considerably inhibited by CST626 (0-10 μM; 96 h) [1].
In vitro, CST626 (0-10 microM; 96 h) shows potent inhibition of cancer cell viability in multiple cancer cell lines. In MOLM13 cells, the IC50 value is 2.1 nM; in SUDHL6 cells, the IC50 value is 1.6 nM. It effectively degrades IAP proteins in a concentration-dependent manner. |
| ln Vivo |
In vivo, CST626 induces DNA damage, promotes apoptosis, and leads to tumor regression in orthotopic WA74 patient-derived xenograft (PDX) models of resistant prostate cancer. It demonstrates significant antitumor efficacy in mouse tumor models, though detailed in vivo protocol data is limited.
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| Enzyme Assay |
CST626 is typically evaluated in non-cellular binding assays to confirm IAP engagement using purified recombinant XIAP, cIAP1, or cIAP2 proteins in a time-resolved FRET (TR-FRET) or AlphaScreen format to measure binding affinity and degradation initiation. For establishing DC50 values, standard degradation assays are performed with protein quantification by western blot.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MM.1S cells Tested Concentrations: 0.0001, 0.001, 0.01, 0.1 and 1 μM Incubation Duration: 16 h Experimental Results: Revealed DC50 values of 2.4 nM(cIAP1), 6.2 nM(cIAP2), and 0.7 nM(XIAP). Cell Viability Assay[1] Cell Types: SUDHL6, MOLM13, NCI-H929, K562, DB, JJN3, HEL, SUDHL4 and RPMI-8826 cells Tested Concentrations: 0.01, 0.04, 0.1, 0.4, 1, 4 and 10 μM Incubation Duration: 96 h Experimental Results: Inhibited cell viability with IC50s of 0.0016, 0.0021, 0.0085, 0.42, 0.46, 1.14, 1.17, 1.69 and 2.54 μM against SUDHL6, MOLM13, NCI-H929, K562, DB, JJN3, H EL, SUDHL4 and RPMI-8826 cells, respectively. For in vitro cellular assays, cells (e.g., MM.1S, MOLM13, or SUDHL6) are seeded in 96-well plates at optimal density. CST626 (0-10 microM range) is added for 48-96 hours. Cell viability is assessed using a luminescent cell viability assay (e.g., CellTiter-Glo). Western blotting is used to measure degradation of XIAP/cIAP1/cIAP2 with beta-actin as loading control. DC50 and IC50 values are calculated from dose-response curves. |
| Animal Protocol |
For in vivo animal efficacy studies, CST626 is typically administered via intraperitoneal injection (e.g., once daily for 14-21 days) at doses of 5-30 mg/kg in mice bearing orthotopic PDX tumors. Tumor volumes are measured twice weekly using calipers. Body weight is monitored to assess tolerability. At study termination, tumors are excised, weighed, and analyzed for IAP degradation by Western blot.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CST626 are those typical of a PROTAC molecule with molecular formula C61H82N8O9S (MW 1103.42). The compound is formulated in solvents like DMSO or PEG400 for in vivo administration. It is recommended to store the powder at -20degC for up to 3 years and in solution at -80degC for 6 months.
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| Toxicity/Toxicokinetics |
In preclinical studies, CST626 shows a favorable safety profile at therapeutic doses. Standard safety pharmacology studies (e.g., hERG, CYP inhibition, and genotoxicity) would be required for clinical development. At high doses, off-target degradation and general cytotoxicity may occur. It is intended for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
CST626 (CAS: 3033993-13-1) is a pan-IAP PROTAC degrader classified under the PROTACs category. Its mechanism of action involves recruiting an E3 ubiquitin ligase to IAP proteins, leading to their ubiquitination and subsequent proteasomal degradation. It is used in cancer research, particularly for apoptosis studies.
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| Molecular Formula |
C61H82N8O9S
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|---|---|
| Molecular Weight |
1103.42
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| Appearance |
White to off-white solid powder
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| SMILES |
O=C([C@H]1N(C([C@H](C2CCCCC2)NC([C@@H](NC)C)=O)=O)C[C@@H](OC3=CC=CC(OCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O)=C3)C1)N[C@@H]7CCCC8=C7C=CC=C8
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~90.6 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (2.27 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (2.27 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9063 mL | 4.5314 mL | 9.0627 mL | |
| 5 mM | 0.1813 mL | 0.9063 mL | 1.8125 mL | |
| 10 mM | 0.0906 mL | 0.4531 mL | 0.9063 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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