| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
The dissociation constant (Kd) of iZMYND8-34 and recombinant ZMYND8-PBP is 1.73 μM[1]. The effect of iZMYND8-34 on luminal C4-2 and 22Rv1 cells is negligible, but it can significantly inhibit the growth of NE1.3 cells, TKO and ST88 organoids[1].
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|---|---|
| ln Vivo |
iZMYND8-34 (10 mg/kg; intraperitoneal injection; once every 2 days; for 6 weeks) can effectively inhibit the development of spontaneous NEPC in TKO mice, prolong survival, reduce tumor burden, and block metastasis [1]. iZMYND8-34 (10 mg/kg; intraperitoneal injection; once every 2 days; for 4 weeks; used in combination with enzalutamide) can effectively inhibit ADT-induced NEPC transdifferentiation in mice, reduce tumor growth, and prolong the survival of LTL-331 PDX model mice [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6 (male; 6 weeks old; genetically engineered: ProbasinCre/+; Ptenflox/flox; Trp53flox/flox; Rb1flox/flox) [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection; every 2 days; for 6 weeks Experimental Results: Significantly prolonged mouse survival (log-rank test, P < 0.0001). Reduced tumor volume in terminal stages. Changed tumor histological type from predominantly neuroendocrine carcinoma (NEPC) to adenocarcinoma or prostatic intraepithelial neoplasia. Eliminated NEPC cell population (CHGA+KRT8-AR- cells). Reduced expression of NE markers (SYP, CHGA). Restored AR expression. Completely prevented metastasis of cancer cells to lymph nodes, lungs, and liver. Animal/Disease Models:NSG (male; 6 weeks old; castrated; subcutaneously implanted with LTL-331 PDX) [1] Doses: 10 mg/kg (in combination with enzalutamide) Route of Administration: Intraperitoneal injection; once every 2 days; for 4 weeks Experimental Results: Significantly inhibited LTL-331 PDX tumor growth. Prolonged mouse survival. Reduced the proportion of CHGA+ NEPC cells. Ki67+ proliferating cells were reduced compared with the vector control group. |
| References |
| Molecular Formula |
C22H19N5O6
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|---|---|
| Molecular Weight |
449.42
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| CAS # |
1358901-59-3
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| Appearance |
White to off-white solid
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| SMILES |
O=C(C1=C2N(C)C(N(C3=CC=C(OCO4)C4=C3)C2=NC(C5=CC=CC(OCC)=C5O)=N1)=O)N
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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 : ~10 mg/mL (~22.25 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (10.0 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 | 2.2251 mL | 11.1255 mL | 22.2509 mL | |
| 5 mM | 0.4450 mL | 2.2251 mL | 4.4502 mL | |
| 10 mM | 0.2225 mL | 1.1125 mL | 2.2251 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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