AT13387 Inhibitor CAS No. 912999-49-6

Cat. No.	Name	Size	Price
KI2609	AT13387	10 mg	$592
	AT13387	25 mg	$1396
	AT13387	50 mg	$1712
	AT13387	100 mg	$2840

Chemical Characteristic

Product Name	AT13387
CAS No.	912999-49-6
Molecular Weight	409.52
Formula	C₂₄H₃₁N₃O₃
Chemical Name	(2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone
Smiles	C(=O)(N1Cc2c(C1)cc(cc2)CN1CCN(CC1)C)c1c(cc(c(c1)C(C)C)O)O
Chemical Structure

Biological activities

AT13387 is a potent and selective inhibitor of Hsp90.[1] The IC50 of AT13387 against Hsp90 is 0.7 nM.^[2] In vitro, AT13387 shows an EC50 of 41?nM and exhibits activity consistent with a cytotoxic effect. In vivo, AT13387 shows low activity against solid tumor and leukemia models of the PPTP.^[3]

Protocols

In vitro, AT13387 is dissolved in DMSO.^[3]

References

[1] Do K, Speranza G, Chen A, et al. Phase I Study Assessing a Two-Consecutive Day (QD x 2) Dosing Schedule of the Hsp90 Inhibitor, AT13387, in Patients with Advanced Solid Tumors. JOURNAL OF CLINICAL ONCOLOGY. 2318 MILL ROAD, STE 800, ALEXANDRIA, VA 22314 USA: AMER SOC CLINICAL ONCOLOGY. 2012, 30 (15). [2] Shapiro G, Kwak E L, Dezube B J, et al. Phase I pharmacokinetic and pharmacodynamic study of the heat shock protein 90 inhibitor AT13387 in patients with refractory solid tumors. J Clin Oncol (Meeting Abstracts). 2010, 28 (15_suppl): 3069. [3] Kang MH, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012, 59 (1):185-188.

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