AMG-510
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MedKoo CAT#: 207085

CAS#: 2252403-56-6

Description: Sotorasib, also known as also known as AMG-510, is a potent KRAS G12C covalent inhibitor and the active atropisomer separated by chiral HPLC. 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. Note: According to Sci-Finder database, CAS#2252403-56-6 is a AMG510 active atropisomer. Many vendor mistakenly listed CAS#2296729-00-3 as the AMG510 active atropisomer.


Chemical Structure

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AMG-510
CAS# 2252403-56-6

Theoretical Analysis

MedKoo Cat#: 207085
Name: AMG-510
CAS#: 2252403-56-6
Chemical Formula: C30H30F2N6O3
Exact Mass: 560.2347
Molecular Weight: 560.61
Elemental Analysis: C, 64.28; H, 5.39; F, 6.78; N, 14.99; O, 8.56

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same day
25.0mg USD 190.0 Same day
50.0mg USD 350.0 Same Day
100.0mg USD 550.0 Same Day
200.0mg USD 950.0 Same Day
500.0mg USD 1950.0 Same Day
1.0g USD 2950.0 2 Weeks
2.0g USD 5150.0 2 Weeks
5.0g USD 7950.0 2 Weeks
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Related CAS #: 2296729-00-3 (racemate)   2252403-56-6   2296729-66-1   2387559-45-5   Unknown (HCl)    

Synonym: AMG-510; AMG 510; AMG510; Sotorasib,

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=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=C2C=C(F)C(C5=C(O)C=CC=C5F)=N4)=O)CC1

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

Preparing Stock Solutions

The following data is based on the product molecular weight 560.61 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

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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.

AMG-510

10.0mg / USD 90.0


Additional Information

AMG 510 can exist in either of two atropisomeric forms and one is more active than the other. It selectively forms an irreversible covalent bond to the sulfur atom in the cysteine residue that is present in the mutated form of KRAS, but not in the normal form.