AZD4877 | potent inhibitor | mitotic spindle kinesin | Eg5 | CAS#1176760-49-8

MedKoo Cat#: 126000 | Name: AZD-4877

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZD4877 is a potent inhibitor of the mitotic spindle kinesin, Eg5.

Chemical Structure

AZD-4877

CAS#1176760-49-8 (free base)

Theoretical Analysis

MedKoo Cat#: 126000

Name: AZD-4877

CAS#: 1176760-49-8 (free base)

Chemical Formula: C28H33N5O2S

Exact Mass: 503.2355

Molecular Weight: 503.67

Elemental Analysis: C, 66.77; H, 6.60; N, 13.91; O, 6.35; S, 6.37

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

758722-12-2 (HCl) 1176760-49-8 (free base)

Synonym

AZD-4877; AZD4877; 1176760-49-8; AZD 4877

IUPAC/Chemical Name

N-(3-aminopropyl)-N-(1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl)-4-methylbenzamide

InChi Key

SMFXSYMLJDHGIE-UHFFFAOYSA-N

InChi Code

InChI=1S/C28H33N5O2S/c1-18(2)24(32(16-8-15-29)27(34)22-13-11-19(3)12-14-22)25-30-26-23(20(4)31-36-26)28(35)33(25)17-21-9-6-5-7-10-21/h5-7,9-14,18,24H,8,15-17,29H2,1-4H3

SMILES Code

CC(C)C(N(CCCN)C(=O)C1=CC=C(C)C=C1)C2=NC3=C(C(C)=NS3)C(=O)N2CC4=CC=CC=C4

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 503.67 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: Gerecitano JF, Stephenson JJ, Lewis NL, Osmukhina A, Li J, Wu K, You Z, Huszar D, Skolnik JM, Schwartz GK. A Phase I trial of the kinesin spindle protein (Eg5) inhibitor AZD4877 in patients with solid and lymphoid malignancies. Invest New Drugs. 2012 May 22. [Epub ahead of print] PubMed PMID: 22615058. 2: Marquis L, Tran M, Choi W, Lee IL, Huszar D, Siefker-Radtke A, Dinney C, McConkey DJ. p63 expression correlates with sensitivity to the Eg5 inhibitor ZD4877 in bladder cancer cells. Cancer Biol Ther. 2012 May 1;13(7):477-86. Epub 2012 May 1. PubMed PMID: 22361733. 3: Theoclitou ME, Aquila B, Block MH, Brassil PJ, Castriotta L, Code E, Collins MP, Davies AM, Deegan T, Ezhuthachan J, Filla S, Freed E, Hu H, Huszar D, Jayaraman M, Lawson D, Lewis PM, Nadella MV, Oza V, Padmanilayam M, Pontz T, Ronco L, Russell D, Whitston D, Zheng X. Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin -6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent. J Med Chem. 2011 Oct 13;54(19):6734-50. Epub 2011 Sep 7. PubMed PMID: 21899292. 4: Esaki T, Seto T, Ariyama H, Arita S, Fujimoto C, Tsukasa K, Kometani T, Nosaki K, Hirai F, Yagawa K. Phase I Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD4877 in Japanese Patients with Solid Tumors. Arch Drug Inf. 2011 Jun;4(2):23-31. PubMed PMID: 21765863; PubMed Central PMCID: PMC3130141. 5: Infante JR, Kurzrock R, Spratlin J, Burris HA, Eckhardt SG, Li J, Wu K, Skolnik JM, Hylander-Gans L, Osmukhina A, Huszar D, Herbst RS. A Phase I study to assess the safety, tolerability, and pharmacokinetics of AZD4877, an intravenous Eg5 inhibitor in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2012 Jan;69(1):165-72. Epub 2011 Jun 3. PubMed PMID: 21638123. 6: Kantarjian HM, Padmanabhan S, Stock W, Tallman MS, Curt GA, Li J, Osmukhina A, Wu K, Huszar D, Borthukar G, Faderl S, Garcia-Manero G, Kadia T, Sankhala K, Odenike O, Altman JK, Minden M. Phase I/II multicenter study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of AZD4877 in patients with refractory acute myeloid leukemia. Invest New Drugs. 2012 Jun;30(3):1107-15. Epub 2011 Apr 15. PubMed PMID: 21494838.