ON012380

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

MedKoo CAT#: 565069

CAS#: 592543-24-3

Description: ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I.

Chemical Structure

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ON012380
CAS# 592543-24-3
Instruction

Theoretical Analysis

MedKoo Cat#: 565069
Name: ON012380
CAS#: 592543-24-3
Chemical Formula: C22H27NO8S
Exact Mass: 465.15
Molecular Weight: 465.520
Elemental Analysis: C, 56.76; H, 5.85; N, 3.01; O, 27.49; S, 6.89

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: ON012380; ON-012380; ON 012380

IUPAC/Chemical Name: N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]-L-alanine

InChi Key: KLFKGEAXNPYTKB-VFNNOXKTSA-N

InChi Code: InChI=1S/C22H27NO8S/c1-14(22(24)25)23-18-10-15(6-7-19(18)29-3)13-32(26,27)9-8-17-20(30-4)11-16(28-2)12-21(17)31-5/h6-12,14,23H,13H2,1-5H3,(H,24,25)/b9-8+/t14-/m0/s1

SMILES Code: C[C@@H](C(O)=O)NC1=CC(CS(=O)(/C=C/C2=C(OC)C=C(OC)C=C2OC)=O)=CC=C1OC

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 465.52 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Wu J, Meng F, Ying Y, Peng Z, Daniels L, Bornmann WG, Quintás-Cardama A, Roulston D, Talpaz M, Peterson LF, Donato NJ. ON012380, a putative BCR-ABL kinase inhibitor with a unique mechanism of action in imatinib-resistant cells. Leukemia. 2010 Apr;24(4):869-72. doi: 10.1038/leu.2009.300. Epub 2010 Jan 28. PubMed PMID: 20111070; PubMed Central PMCID: PMC4677994.

2: Maekawa T, Ashihara E, Kimura S. The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias. Int J Clin Oncol. 2007 Oct;12(5):327-40. Epub 2007 Oct 22. Review. PubMed PMID: 17929114.

3: Kimura S, Ashihara E, Maekawa T. New tyrosine kinase inhibitors in the treatment of chronic myeloid leukemia. Curr Pharm Biotechnol. 2006 Oct;7(5):371-9. Review. PubMed PMID: 17076652.

4: Tauchi T, Ohyashiki K. The second generation of BCR-ABL tyrosine kinase inhibitors. Int J Hematol. 2006 May;83(4):294-300. Review. PubMed PMID: 16757427.

5: Walz C, Sattler M. Novel targeted therapies to overcome imatinib mesylate resistance in chronic myeloid leukemia (CML). Crit Rev Oncol Hematol. 2006 Feb;57(2):145-64. Epub 2005 Oct 5. Review. PubMed PMID: 16213151.

6: Gumireddy K, Baker SJ, Cosenza SC, John P, Kang AD, Robell KA, Reddy MV, Reddy EP. A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance. Proc Natl Acad Sci U S A. 2005 Feb 8;102(6):1992-7. Epub 2005 Jan 27. Erratum in: Proc Natl Acad Sci U S A. 2005 Apr 12;102(15):5635. PubMed PMID: 15677719; PubMed Central PMCID: PMC546016.