UC2288

Product NameUC2288
CAS1394011-91-6
MFC20H18ClF6N3O2
MW481.82
EINECS
MOL File1394011-91-6.mol

Chemical Properties

Melting point	176.5-177.9 °C(Solvent: Methanol)
Boiling point	491.9±45.0 °C(Predicted)
Density	1.45±0.1 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMF: 25 mg/ml; DMSO: 25 mg/ml; Ethanol: 25 mg/ml
form	A solid
pka	12.88±0.40(Predicted)
color	White to off-white
InChIKey	ISPSOOYSNVVMMB-MQMHXKEQSA-N
SMILES	O=C(N[C@@H]1CC[C@@H](OC2=CC=C(C=N2)C(F)(F)F)CC1)NC3=CC(C(F)(F)F)=C(Cl)C=C3

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM[1].

Biological Activity

Cell permeable: yes

in vivo

UC2888 (oral gavage; 15 mg/kg; 3 times a week; 4 weeks) co-treatment with imetelstat significantly suppresses tumor growth and does not effect mice weight^[2].UC2288 (intraperitoneal injection; 10 mg/kg; 4 times in 7 days) attenuates MPTP-induced behavioral impairment, prevents activation of MAPK pathway in the MPTP-treated mice brain. MPTP treatment raises TNF-α, IL-6 and IL-1β levels in MPTP treated mice brain, but UC2288 signicantly decreases MPTP-induced TNF-α, IL-6 levels, but IL-1β is not decreased in brain^[3].

Animal Model:	Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x10⁶)^[2]
Dosage:	15 mg/kg
Administration:	Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result:	Combined treatment with imetelstat synergistically inhibited tumor growth in mice.

Animal Model:	MPTP-induced C57BL6 Parkinson’s disease mice model^[3]
Dosage:	10 mg/kg
Administration:	Intraperitonealinjection; 4 times in 7 days
Result:	Ameliorated MPTP induced PD progression through inhibition of neuroinammation.

References

[1] Hiromi I Wettersten, et al. A Novel p21 Attenuator Which Is Structurally Related to Sorafenib. Cancer Biol Ther.2013 Mar;14(3):278-85. DOI:10.4161/cbt.23374
[2] Romi Gupta, et al. Synergistic tumor suppression by combined inhibition of telomerase and CDKN1A. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):E3062-71. DOI:10.1073/pnas.1411370111
[3] Jun Hyung Im, et al. p21 inhibitor UC2288 ameliorates MPTP induced Parkinson’s disease progression through inhibition of oxidative stress and neuroinammation. Translational Medicine.Neurobiology of Disease

UC2288 Supplier

UC2288 manufacturers

Related Product Information

Send Inquriy