RGB-286638 free base
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MedKoo CAT#: 206738

CAS#: 784210-88-4 (free base)

Description: RGB-286638 is a multitargeted cyclin-dependent kinase inhibitor. RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. GB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo. RGB-286638 displayed caspase-dependent apoptosis in both wt-p53 and mutant-p53 cells that was closely associated with the downregulation of RNA polymerase II phosphorylation and inhibition of transcription. RGB-286638 triggered p53 accumulation via nucleolar stress and loss of Mdm2, accompanied by induction of p53 DNA-binding activity.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 2 Weeks
25mg USD 250 2 Weeks
50mg USD 450 2 Weeks
100mg USD 650 2 Weeks
200mg USD 1050 2 Weeks
500mg USD 1850 2 Weeks
1g USD 2950 2 Weeks
2g USD 4250 2 Weeks
5g USD 7450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-23. Prices are subject to change without notice.

RGB-286638 free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206738
Name: RGB-286638 free base
CAS#: 784210-88-4 (free base)
Chemical Formula: C29H35N7O4
Exact Mass: 545.2751
Molecular Weight: 545.644
Elemental Analysis: C, 63.84; H, 6.47; N, 17.97; O, 11.73


Related CAS #: 784210-87-3 (dihydrochloride)   784210-88-4 (free base)  

Synonym: RGB-286638, RGB 286638, RGB286638; RGB-286638 free base

IUPAC/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

InChi Key: XLSYZSRXVVCHLS-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

Related CAS#
784210-87-3 (RGB-286638 dihydrochloride)
784210-88-4 (RGB-286638 free base)


References

1: Morales F, Giordano A. Overview of CDK9 as a target in cancer research. Cell Cycle. 2016;15(4):519-27. doi: 10.1080/15384101.2016.1138186. PubMed PMID: 26766294.

2: Aleem E, Arceci RJ. Targeting cell cycle regulators in hematologic malignancies. Front Cell Dev Biol. 2015 Apr 9;3:16. doi: 10.3389/fcell.2015.00016. eCollection 2015. Review. PubMed PMID: 25914884; PubMed Central PMCID: PMC4390903.

3: van der Biessen DA, Burger H, de Bruijn P, Lamers CH, Naus N, Loferer H, Wiemer EA, Mathijssen RH, de Jonge MJ. Phase I study of RGB-286638, a novel, multitargeted cyclin-dependent kinase inhibitor in patients with solid tumors. Clin Cancer Res. 2014 Sep 15;20(18):4776-83. doi: 10.1158/1078-0432.CCR-14-0325. Epub 2014 Jul 14. PubMed PMID: 25024258.

4: Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G, Ohguchi H, Suzuki R, Loferer H, Munshi NC, Anderson KC, Raje N. 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. doi: 10.1038/leu.2013.194. Epub 2013 Jun 28. PubMed PMID: 23807770; PubMed Central PMCID: PMC3928098.

5: de Bruijn P, Moghaddam-Helmantel IM, de Jonge MJ, Meyer T, Lam MH, Verweij J, Wiemer EA, Loos WJ. Validated bioanalytical method for the quantification of RGB-286638, a novel multi-targeted protein kinase inhibitor, in human plasma and urine by liquid chromatography/tandem triple-quadrupole mass spectrometry. J Pharm Biomed Anal. 2009 Dec 5;50(5):977-82. doi: 10.1016/j.jpba.2009.06.048. Epub 2009 Jul 7. PubMed PMID: 19628352.