| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
IC50: 0.68 μM (HT29); 0.6 μM (OVCAR-3); 16 μM (AsPC-1); 0.14 μM (PC-3)
|
|---|---|
| ln Vitro |
LP-184 possesses GI50s of 0.68, 0.6, 16, and 0.14 μM, which indicate its ability to suppress the development of HT29, OVCAR-3, AsPC-1, and PC-3, respectively. In the 72-hour Trypan blue assay and the 2-hour thymidine incorporation into cellular DNA assay, LP-184 exhibits anti-cancer activity with IC50s of 800 nM and 210 nM, respectively[1].
|
| ln Vivo |
LP-184 (7.5 and 10 mg/kg; ip; 21 day) provides strong 15 anti-tumor activity against MV522 tumors, resulting in 4/6 and 5/5 partial responses, in that order[1].
|
| Animal Protocol |
Animal/Disease Models: Mice (MV522 tumors )[1]
Doses: 7.5 and 10 mg/kg Route of Administration: Ip; 21day Experimental Results: Effective agent for human anti-tumor therapy. |
| References | |
| Additional Infomation |
Acylfulvene-derived Prodrug LP-184 is a tumor-site activated acylfulvene-derived prodrug and alkylating agent, with potential antineoplastic activity. Upon administration, acylfulvene-derived prodrug LP-184 becomes activated by prostaglandin reductase 1 (PTGR1), an oxidoreductase that is specifically upregulated in certain tumor cell types. The active form of LP-184 covalently binds to and alkylates DNA at N3-adenine, thereby causing double strand breaks. As tumor cells often carry DNA damage repair (DDR) mutations and are therefore deficient in DDR pathways, the DNA damage cannot be repaired. In turn, the damaged DNA causes apoptosis and inhibits proliferation in susceptible DDR mutated tumor cells. PTGR1 is often elevated in solid tumors but not in normal tissues.
|
| Molecular Formula |
C16H20N2O4
|
|---|---|
| Molecular Weight |
304.34
|
| Exact Mass |
304.142
|
| CAS # |
924835-67-6
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| Related CAS # |
LP-284;2412580-47-1
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| PubChem CID |
15945880
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
-1.1
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
|
| Complexity |
697
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
N(CC1C2C(=CC=1C)C(=O)[C@@](O)(C)C1(C=2C)CC1)(O)C(N)=O
|
| InChi Key |
VWMPVAZEBAKLFR-HNNXBMFYSA-N
|
| InChi Code |
InChI=1S/C16H20N2O4/c1-8-6-10-12(11(8)7-18(22)14(17)20)9(2)16(4-5-16)15(3,21)13(10)19/h6,21-22H,4-5,7H2,1-3H3,(H2,17,20)/t15-/m0/s1
|
| Chemical Name |
1-hydroxy-1-[[(5'R)-5'-hydroxy-2',5',7'-trimethyl-4'-oxospiro[cyclopropane-1,6'-indene]-1'-yl]methyl]urea
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (328.58 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.21 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 25.0 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: ≥ 2.5 mg/mL (8.21 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2858 mL | 16.4290 mL | 32.8580 mL | |
| 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL | |
| 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 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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