WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407878
Description: IIIM-290 is a potent and Orally Active Cyclin-dependent Kinase Inhibitor. IIIM-290 showed strong inhibition of Cdk-9/T1 (IC50 1.9 nM) kinase and Molt-4/MIAPaCa-2 cell growth (GI50 < 1.0 µM) and was found to be highly selective for cancer cells over normal fibroblast-cells. It inhibited the cell growth of MIAPaCa-2 cells via caspase-dependent apoptosis. IIIM-290 achieved 71% oral bioavailability with in-vivo efficacy in pancreatic, colon and leukemia xenografts at 50 mg/kg, po. IIIM-290 did not have CYP/ efflux-pump liability, was not mutagenic/genotoxic or cardiotoxic and was metabolically-stable.
MedKoo Cat#: 407878
Chemical Formula: C23H21Cl2NO5
Exact Mass: 461.0797
Molecular Weight: 462.323
Elemental Analysis: C, 59.75; H, 4.58; Cl, 15.34; N, 3.03; O, 17.30
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 1632143-39-5 (racemic free base) 1632143-49-7 (racemic HCl)
Synonym: IIIM-290; IIIM 290; IIIM290.
IUPAC/Chemical Name: 2-((E)-2,6-dichlorostyryl)-5,7-dihydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4H-chromen-4-one
InChi Key: NFTJDXGFOUFNKG-UGBNQVSOSA-N
InChi Code: InChI=1S/C23H21Cl2NO5/c1-26-8-7-14(20(30)11-26)21-18(28)10-19(29)22-17(27)9-12(31-23(21)22)5-6-13-15(24)3-2-4-16(13)25/h2-6,9-10,14,20,28-30H,7-8,11H2,1H3/b6-5+/t14-,20+/m0/s1
SMILES Code: O=C1C=C(/C=C/C2=C(Cl)C=CC=C2Cl)OC3=C1C(O)=CC(O)=C3[C@@H]4[C@H](O)CN(C)CC4
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
The following data is based on the product molecular weight 462.323 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Bharate SB, Kumar V, Jain SK, Mintoo MJ, Guru SK, Nuthakki VK, Sharma M,
Bharate SS, Gandhi SG, Mondhe DM, Bhushan S, Vishwakarma RA. Discovery and
Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-dependent
Kinase Inhibitor. J Med Chem. 2018 Jan 25. doi: 10.1021/acs.jmedchem.7b01765.
[Epub ahead of print] PubMed PMID: 29370702.