| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
KW-2478 (KW 2478; KW2478) is a nonansamycin inhibitor of HSP90 (Heat Shock Protein 90) with potential antitumor activity. It inhibits HSP90 with an IC50 of 3.8 nM. It demonstrates significant in vivo antitumor efficacy in NCI-H929 tumor-bearing SCID mice.
| ln Vitro |
Hsp90 inhibition: KW-2478 has an IC50 of 3.8 nM for Hsp90α. For both non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM), KW-2478 exhibits anti-proliferative action. Its GI50 values are 0.30 μM (OPM-2 /GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM μM (SC-1). By primarily inhibiting the activity of Cdk9, KW -2478 also suppresses the transcription of the c-Maf and Cyclin D1 genes[1].
|
||
|---|---|---|---|
| ln Vivo |
In combined immunodeficiency (SCID) mice carrying NCI-H929 cells, KW-2478 (25-200 mg/kg, iv) suppresses tumor growth without causing body weight loss. Mice NCI-H929 tumors treated with KW-2478 (100 mg/kg, IV) show dephosphorylated Erk1/2 proteins and Hsp90 client protein levels being degraded[1].
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C30H42N2O9
|
|---|---|
| Molecular Weight |
574.66
|
| Exact Mass |
574.289
|
| CAS # |
819812-04-9
|
| Related CAS # |
819812-18-5 (HCl);819812-04-9;
|
| PubChem CID |
23116322
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
746.9±60.0 °C at 760 mmHg
|
| Flash Point |
405.5±32.9 °C
|
| Vapour Pressure |
0.0±2.6 mmHg at 25°C
|
| Index of Refraction |
1.560
|
| LogP |
2.99
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
16
|
| Heavy Atom Count |
41
|
| Complexity |
773
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
VFUXSYAXEKYYMB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C30H42N2O9/c1-5-22-23(19-28(35)32(11-13-37-2)12-14-38-3)29(25(34)20-24(22)33)30(36)21-6-7-26(27(18-21)39-4)41-17-10-31-8-15-40-16-9-31/h6-7,18,20,33-34H,5,8-17,19H2,1-4H3
|
| Chemical Name |
2-(2-ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxyethyl)acetamide
|
| Synonyms |
KW-2478; KW2478; KW 2478.
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.70 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 50.0 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: ≥ 5 mg/mL (8.70 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 50.0 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. View More
Solubility in Formulation 3: ≥ 5 mg/mL (8.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W: 10mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7402 mL | 8.7008 mL | 17.4016 mL | |
| 5 mM | 0.3480 mL | 1.7402 mL | 3.4803 mL | |
| 10 mM | 0.1740 mL | 0.8701 mL | 1.7402 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00457782 | Completed | Drug: KW-2478 | Multiple Myeloma Chronic Lymphocytic Leukaemia |
Kyowa Hakko Kirin UK, Ltd. | April 2007 | Phase 1 |
| NCT01063907 | Completed Has Results | Drug: KW-2478 Drug: Bortezomib |
Multiple Myeloma | Kyowa Hakko Kirin Pharma, Inc. | March 2010 | Phase 1 Phase 2 |
|
|---|
|
|
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
