MedKoo Cat#: 573535 | Name: AT-9283 L-lactate
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Description:

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

AT-9283 is a small-molecule multi-targeted kinase inhibitor with potent bioactivity against Aurora A and B kinases, JAK2, JAK3, and Abl kinases. It exhibits IC₅₀ values of 3 nM for Aurora B, 21 nM for Aurora A, 1.2 nM for JAK2, 1.1 nM for JAK3, and approximately 3 nM for Abl (including the T315I mutant). In preclinical cancer models, AT-9283 induces polyploidy and apoptosis in tumor cells due to mitotic disruption from Aurora inhibition, and demonstrates antiproliferative effects across a range of hematologic malignancies and solid tumors. It has shown in vivo efficacy in xenograft models and entered early-phase clinical trials, though dose-limiting toxicities such as neutropenia were observed.

Chemical Structure

AT-9283 L-lactate
AT-9283 L-lactate
CAS#896466-76-5 (lactate)

Theoretical Analysis

MedKoo Cat#: 573535

Name: AT-9283 L-lactate

CAS#: 896466-76-5 (lactate)

Chemical Formula: C22H29N7O5

Exact Mass: 0.0000

Molecular Weight: 471.52

Elemental Analysis: C, 56.04; H, 6.20; N, 20.79; O, 16.97

Price and Availability

Size Price Availability Quantity
100mg USD 850.00 2 Weeks
200mg USD 1,450.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 3,250.00 2 Weeks
2g USD 5,450.00 2 Weeks
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Synonym
AT-9283 L-lactate; AT-9283; AT 9283; AT9283
IUPAC/Chemical Name
Propanoic acid, 2-hydroxy-, (2S)-, compd. with N-cyclopropyl-N'-(3-(6-(4-morpholinylmethyl)-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl)urea (1:1)
InChi Key
RWYNKTMXFIMBFE-WNQIDUERSA-N
InChi Code
1S/C19H23N7O2.C3H6O3/c27-19(21-13-2-3-13)24-16-10-20-25-17(16)18-22-14-4-1-12(9-15(14)23-18)11-26-5-7-28-8-6-26;1-2(4)3(5)6/h1,4,9-10,13H,2-3,5-8,11H2,(H,20,25)(H,22,23)(H2,21,24,27);2,4H,1H3,(H,5,6)/t;2-/m.0/s1
SMILES Code
C[C@H](O)C(=O)O.O=C(NC1CC1)Nc2c[nH]nc2c3nc4cc(CN5CCOCC5)ccc4[nH]3
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
>3 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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 471.52 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.

Recalculate based on batch purity %
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: Duong JK, Griffin MJ, Hargrave D, Vormoor J, Edwards D, Boddy AV. A population pharmacokinetic model of AT9283 in adults and children to predict the maximum tolerated dose in children with leukaemia. Br J Clin Pharmacol. 2017 Aug;83(8):1713-1722. doi: 10.1111/bcp.13260. Epub 2017 Mar 5. PubMed PMID: 28177130; PubMed Central PMCID: PMC5510070. 2: Vormoor B, Veal GJ, Griffin MJ, Boddy AV, Irving J, Minto L, Case M, Banerji U, Swales KE, Tall JR, Moore AS, Toguchi M, Acton G, Dyer K, Schwab C, Harrison CJ, Grainger JD, Lancaster D, Kearns P, Hargrave D, Vormoor J. A phase I/II trial of AT9283, a selective inhibitor of aurora kinase in children with relapsed or refractory acute leukemia: challenges to run early phase clinical trials for children with leukemia. Pediatr Blood Cancer. 2017 Jun;64(6). doi: 10.1002/pbc.26351. Epub 2016 Dec 1. PubMed PMID: 27905678. 3: Hay AE, Murugesan A, DiPasquale AM, Kouroukis T, Sandhu I, Kukreti V, Bahlis NJ, Lategan J, Reece DE, Lyons JF, Sederias J, Xu H, Powers J, Seymour LK, Reiman T. A phase II study of AT9283, an aurora kinase inhibitor, in patients with relapsed or refractory multiple myeloma: NCIC clinical trials group IND.191. Leuk Lymphoma. 2016;57(6):1463-6. doi: 10.3109/10428194.2015.1091927. Epub 2015 Oct 15. PubMed PMID: 26376958. 4: Moawad EY. Optimizing and predicting the in vivo activity of AT9283 as a monotherapy and in combination with paclitaxel. J Gastrointest Cancer. 2015 Dec;46(4):380-9. doi: 10.1007/s12029-015-9761-9. PubMed PMID: 26346504. 5: Qi W, Liu X, Cooke LS, Persky DO, Miller TP, Squires M, Mahadevan D. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005. doi: 10.1002/ijc.26324. Epub 2011 Nov 19. PubMed PMID: 21796626.