LDE225 Inhibitor CAS No. 956697-53-3

Cat. No.	Name	Size	Price
KI0483	LDE225	5 mg	$240
	LDE225	10 mg	$432
	LDE225	25 mg	$752
	LDE225	50 mg	$1120

Chemical Characteristic

Product Name	LDE225
Synonyms	NVP-LDE225, Erismodegib
CAS No.	956697-53-3
Molecular Weight	485.5
Formula	C₂₆H₂₆F₃N₃O₃
Chemical Name	rel-N-[6-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-[1,1'-biphenyl]-3-carboxamide
Smiles	c1(c(c(ccc1)C(=O)Nc1cnc(cc1)N1C[C@H](O[C@H](C1)C)C)C)c1ccc(cc1)OC(F)(F)F
Chemical Structure
Documents	HPLC MS COA

Biological activities

LDE225 is a potent and selective smoothened antagonist. The IC50 values of LDE225 against mouse smoothened (Smo) and human Smo are 1.3 and 2.5 nM, respectively. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species (mouse, rat, dog and monkey) when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility.^[1] LDE225 combining with nilotinib inhibits the chronic myeloid leukemia stem cells. LDE-225 also inhibits human prostate cancer stem cell growth in NOD/SCID IL2Rγ null mice. In vitro, LDE225 treatment also increases sensitivity of ALDH-positive cells to paclitaxel. Chemotherapy-resistant ovarian cancer cell lines (A2780cp20 and SKOV3TRip2) xenografts treated with combined LDE225 and paclitaxel has significantly less tumor burden than those treated with vehicle or either LDE225 alone.^[2] In a transgenic mouse model of islet cell neoplasms, LDE225 (80 mg/kg) significantly reduces tumor volume by 95% compared with untreated control mice. Hedgehog inhibition with LDE225 also significantly prolongs median survival in the used transgenic mouse model.^[3] In the subcutaneous Ptch+/-p53-/-medulloblastoma allograft mouse model, LDE225 demonstrates dose-related antitumor activity. When dosed at a dose of 5mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. Besides, LDE225 can successfully penetrates the blood-brain barrier in tumor-bearing animals. ^[1]

Protocols

In vitro: LDE225 is dissolved in DMSO.^[2]

References

[1] Shifeng Pan, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med. Chem. Lett. 2010, 1 (3), pp 130-134. [2] Steg AD, et al. Smoothened antagonists reverse taxane resistance in ovarian cancer. Mol Cancer Ther. 2012, 11(7): 1587-1597. [3] Fendrich V, et al. Hedgehog inhibition with the orally bioavailable Smo antagonist LDE225 represses tumor growth and prolongs survival in a transgenic mouse model of islet cell neoplasms. Ann Surg. 2011, 254(5): 818-823

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