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BTdCPU is an activator of HRI (heme-regulated eIF2α kinase) with anticancer activity. It has the ability to induce apoptosis in resistant cells and promote phosphorylation of eIF2α. In multiple myeloma, the eIF2-alpha kinase HRI is a novel therapeutic target. In dex-resistant cells, combination therapy utilizing BTdCPU, an HRI activator, and rapamycin, an mTOR inhibitor, showed additive effects on apoptosis. Therefore, targeted activation of the eIF2α kinase HRI represents a new therapeutic target for MM that can complement existing therapeutic approaches.
| Targets |
HRI
|
|---|---|
| ln Vitro |
BTdCPU (10 μM; 4, 8 h) BTdCPU causes eIF2α phosphorylation and encourages MM cell death [1]. Dex-resistant primary MM cells are cytotoxic to BTdCPU (10 μM; 4, 8 h) [1].
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| ln Vivo |
In a mouse xenograft mammary tumor model, BTdCPU (175 mg/kg; intraperitoneal injection; once daily for 21 days) suppresses tumor growth without causing toxicity [2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Bone marrow mononuclear cells (MNC) from multiple myeloma (MM) patients or healthy donors Tested Concentrations: 10 μM Incubation Duration: 0, 4, 8 hrs (hours) Experimental Results: In MM patient cells Induces early expression of CHOP but not in healthy bone marrow mononuclear cells (MNC). |
| Animal Protocol |
Animal/Disease Models: Female nude mouse (mouse xenograft mammary tumor model) [2].
Doses: 175 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 21 days Experimental Results: Experimental Results:Complete tumor stasis that persisted for the remainder of the 3-week study, showing good safety in mice. |
| References |
| Molecular Formula |
C13H8CL2N4OS
|
|---|---|
| Molecular Weight |
339.199818611145
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| Exact Mass |
337.98
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| Elemental Analysis |
C, 46.03; H, 2.38; Cl, 20.90; N, 16.52; O, 4.72; S, 9.45
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| CAS # |
1257423-87-2
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| Related CAS # |
1257423-87-2
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| PubChem CID |
49787174
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| Appearance |
White to off-white solid powder
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| Density |
1.664±0.06 g/cm3(Predicted)
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C=CC(=C1)NC(NC1=CC=C2C(=C1)SN=N2)=O)Cl
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| InChi Key |
NUUSUAWULNXMGF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8Cl2N4OS/c14-9-3-1-7(5-10(9)15)16-13(20)17-8-2-4-11-12(6-8)21-19-18-11/h1-6H,(H2,16,17,20)
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| Chemical Name |
1-(1,2,3-benzothiadiazol-6-yl)-3-(3,4-dichlorophenyl)urea
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| Synonyms |
BTdCPU
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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: 68~125 mg/mL (200.4~368.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (6.13 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 can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9481 mL | 14.7406 mL | 29.4811 mL | |
| 5 mM | 0.5896 mL | 2.9481 mL | 5.8962 mL | |
| 10 mM | 0.2948 mL | 1.4741 mL | 2.9481 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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