AMG510 HCl

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

MedKoo CAT#: 532729

CAS#: Unknown (HCl)

Description: AMG-510 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. 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

img
AMG510 HCl
CAS# Unknown (HCl)

Theoretical Analysis

MedKoo Cat#: 532729
Name: AMG510 HCl
CAS#: Unknown (HCl)
Chemical Formula: C30H31ClF2N6O3
Exact Mass: 560.2347
Molecular Weight: 597.06
Elemental Analysis: C, 60.35; H, 5.23; Cl, 5.94; F, 6.36; N, 14.08; O, 8.04

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

Related CAS #: 2296729-00-3 (racemate)   2252403-56-6   2296729-66-1   2387559-45-5   Unknown (HCl)    

Synonym: AMG510; AMG-510; AMG 510; AMG510 HCl; AMG510 hydrochloride;

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 hydrochloride

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.[H]Cl

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 597.06 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.