RGB-286638 free baseCAS# 784210-88-4 |
- RG7388
Catalog No.:BCC1895
CAS No.:1229705-06-9
- MI-773
Catalog No.:BCC5155
CAS No.:1303607-07-9
- Nutlin-3a chiral
Catalog No.:BCC1812
CAS No.:675576-98-4
- MIRA-1
Catalog No.:BCC2409
CAS No.:72835-26-8
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 784210-88-4 | SDF | Download SDF |
PubChem ID | 11285002 | Appearance | Powder |
Formula | C29H35N7O4 | M.Wt | 545.63 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : ≥ 36 mg/mL (65.98 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-ylurea | ||
SMILES | COCCN1CCN(CC1)CC2=CC=C(C=C2)C3=NNC4=C3C(=O)C5=C4C=CC=C5NC(=O)NN6CCOCC6 | ||
Standard InChIKey | XLSYZSRXVVCHLS-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C29H35N7O4/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
RGB-286638 free base Dilution Calculator
RGB-286638 free base Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.8327 mL | 9.1637 mL | 18.3274 mL | 36.6549 mL | 45.8186 mL |
5 mM | 0.3665 mL | 1.8327 mL | 3.6655 mL | 7.331 mL | 9.1637 mL |
10 mM | 0.1833 mL | 0.9164 mL | 1.8327 mL | 3.6655 mL | 4.5819 mL |
50 mM | 0.0367 mL | 0.1833 mL | 0.3665 mL | 0.7331 mL | 0.9164 mL |
100 mM | 0.0183 mL | 0.0916 mL | 0.1833 mL | 0.3665 mL | 0.4582 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
In Vitro:RGB-286638 is an indenopyrazole-derived CDK inhibitor (CDKI) with Ki-nanomolar activity against transcriptional CDKs. RGB-286638 inhibits several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. The dose- and time-dependent effect of treatment with RGB-286638 (12.5-100nM) is investigated on the growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells by MTT assay, assessing viability at 24 and 48 hours. The half-maximally effective concentrations (EC50) range between 20 and 70 nM at 48 hours. Dose-dependent differences in growth among p53-wt and -mutant cells are observed after 50nM treatment, with p53-wt MM.1S, MM.1R and H929 being slightly more sensitive to RGB-286638 treatment at 48h[1].
In Vivo:Dose-finding studies with RGB-286638 identify 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppresses MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% and 86.34% in the 30 mg/kg and 40 mg/kg treated cohorts respectively. The log10 cell kill (LCK Td: 4.5 days) is 1.6 for both treated groups. RGB-286638 treatment is also associated with improved survival, evidenced by first death at day 24 in controls versus day 43 in both treated groups. No toxic deaths occurred during this study: maximum percentage of body weight (BW) loss is observed on day 5 (8.4%) at 30 mg/kg dosage schedule, and on day 15 (9.9%) after 40 mg/kg dosing, with weight recovery in the following two weeks[1].
References:
[1]. Cirstea D, et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.
- RGB-286638
Catalog No.:BCC5519
CAS No.:784210-87-3
- 5,7,3'-Trihydroxy-6,4',5'-trimethoxyflavone
Catalog No.:BCN1353
CAS No.:78417-26-2
- Trequinsin hydrochloride
Catalog No.:BCC7333
CAS No.:78416-81-6
- Milrinone
Catalog No.:BCC4374
CAS No.:78415-72-2
- 1,7-Dihydroxy-2,3-dimethoxyxanthone
Catalog No.:BCN7523
CAS No.:78405-33-1
- MY-5445
Catalog No.:BCC6645
CAS No.:78351-75-4
- Pyranojacareubin
Catalog No.:BCN7429
CAS No.:78343-62-1
- Nocamycin I
Catalog No.:BCN1845
CAS No.:78339-49-8
- PCI-24781 (CRA-024781)
Catalog No.:BCC2155
CAS No.:783355-60-2
- MLN120B
Catalog No.:BCC1772
CAS No.:783348-36-7
- MRK 016
Catalog No.:BCC6070
CAS No.:783331-24-8
- H-D-1-Nal-OH
Catalog No.:BCC3281
CAS No.:78306-92-0
- Deacetyltaxol
Catalog No.:BCN2820
CAS No.:78432-77-6
- 19-Hydroxybaccatin III
Catalog No.:BCN4330
CAS No.:78432-78-7
- 7-Epi 10-Desacetyl Paclitaxel
Catalog No.:BCC1314
CAS No.:78454-17-8
- Enterolakton
Catalog No.:BCC8170
CAS No.:78473-71-9
- Praeruptorin E
Catalog No.:BCN2591
CAS No.:78478-28-1
- 7-Epi-10-deacetylcephalomannine
Catalog No.:BCN7673
CAS No.:78479-12-6
- N-trans-Feruloyl-3-methoxytyramine
Catalog No.:BCN4331
CAS No.:78510-19-7
- PSB 069
Catalog No.:BCC7416
CAS No.:78510-31-3
- Asperumine
Catalog No.:BCN2039
CAS No.:78513-20-9
- Dulcioic acid
Catalog No.:BCN4579
CAS No.:78516-69-5
- Excisanin B
Catalog No.:BCN4332
CAS No.:78536-36-4
- Excisanin A
Catalog No.:BCN7643
CAS No.:78536-37-5