AMG-510 racemate
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MedKoo CAT#: 207099

CAS#: 2296729-00-3 (racemate)

Description: AMG-510 racemate is a racemic mixture of AMB-510, which is a potent KRAS G12C covalent inhibitor. AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells


Price and Availability

Size Price Shipping out time Quantity
100mg USD 950 2 Weeks
200mg USD 1750 2 Weeks
500mg USD 2850 2 Weeks
1g USD 3950 2 Weeks
2g USD 7250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-06-05. Prices are subject to change without notice.

AMG-510 racemate, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 207099
Name: AMG-510 racemate
CAS#: 2296729-00-3 (racemate)
Chemical Formula: C30H30F2N6O3
Exact Mass: 560.2347
Molecular Weight: 560.6058
Elemental Analysis: C, 64.28; H, 5.39; F, 6.78; N, 14.99; O, 8.56


Related CAS #: 2296729-00-3 (racemate)   2252403-56-6    

Synonym: AMG-510 racemate; AMG 510; AMG-510; AMG510;

IUPAC/Chemical Name: 4-((S)-4-acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one

InChi Key: NXQKSXLFSAEQCZ-SFHVURJKSA-N

InChi Code: InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3/t18-/m0/s1

SMILES Code: O=C1N(C2=C(C)C=CN=C2C(C)C)C3=NC(C4=C(O)C=CC=C4F)=C(F)C=C3C(N5[C@@H](C)CN(C(C=C)=O)CC5)=N1


Technical Data

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


References

1: Ryan MB, Fece de la Cruz F, Phat S, Myers DT, Wong E, Shahzade HA, Hong CB, Corcoran RB. Vertical pathway inhibition overcomes adaptive feedback resistance to KRASG12C inhibition. Clin Cancer Res. 2019 Nov 27. pii: clincanres.3523.2019. doi: 10.1158/1078-0432.CCR-19-3523. [Epub ahead of print] PubMed PMID: 31776128.

2: Canon J, Rex K, Saiki AY, Mohr C, Cooke K, Bagal D, Gaida K, Holt T, Knutson CG, Koppada N, Lanman BA, Werner J, Rapaport AS, San Miguel T, Ortiz R, Osgood T, Sun JR, Zhu X, McCarter JD, Volak LP, Houk BE, Fakih MG, O'Neil BH, Price TJ, Falchook GS, Desai J, Kuo J, Govindan R, Hong DS, Ouyang W, Henary H, Arvedson T, Cee VJ, Lipford JR. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223. doi: 10.1038/s41586-019-1694-1. Epub 2019 Oct 30. PubMed PMID: 31666701.

3: AMG 510 First to Inhibit "Undruggable" KRAS. Cancer Discov. 2019 Aug;9(8):988-989. doi: 10.1158/2159-8290.CD-NB2019-073. Epub 2019 Jun 12. PubMed PMID: 31189530.

4: Aoude LG, Pritchard AL, Robles-Espinoza CD, Wadt K, Harland M, Choi J, Gartside M, Quesada V, Johansson P, Palmer JM, Ramsay AJ, Zhang X, Jones K, Symmons J, Holland EA, Schmid H, Bonazzi V, Woods S, Dutton-Regester K, Stark MS, Snowden H, van Doorn R, Montgomery GW, Martin NG, Keane TM, López-Otín C, Gerdes AM, Olsson H, Ingvar C, Borg A, Gruis NA, Trent JM, Jönsson G, Bishop DT, Mann GJ, Newton-Bishop JA, Brown KM, Adams DJ, Hayward NK. Nonsense mutations in the shelterin complex genes ACD and TERF2IP in familial melanoma. J Natl Cancer Inst. 2014 Dec 13;107(2). pii: dju408. doi: 10.1093/jnci/dju408. Print 2015 Feb. PubMed PMID: 25505254; PubMed Central PMCID: PMC4334787.

5: Andrews DA, Pyrah IT, Boren BM, Tannehill-Gregg SH, Lightfoot-Dunn RM. High hematocrit resulting from administration of erythropoiesis-stimulating agents is not fully predictive of mortality or toxicities in preclinical species. Toxicol Pathol. 2014;42(3):510-23. doi: 10.1177/0192623313486317. Epub 2013 May 14. Review. PubMed PMID: 23674390.

6: Iidaka T, Miyakoshi M, Harada T, Nakai T. White matter connectivity between superior temporal sulcus and amygdala is associated with autistic trait in healthy humans. Neurosci Lett. 2012 Feb 29;510(2):154-8. doi: 10.1016/j.neulet.2012.01.029. Epub 2012 Jan 25. PubMed PMID: 22285821.

7: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Apr;28(3):185-206. PubMed PMID: 16810345.