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MedKoo Cat#: 207085 | Name: Sotorasib (AMG-510)
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Description:

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

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

Sotorasib (AMG-510)
CAS#2252403-56-6

Theoretical Analysis

MedKoo Cat#: 207085

Name: Sotorasib (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
5mg USD 90.00 Ready to ship
50mg USD 150.00 Ready to ship
100mg USD 250.00 Ready to ship
200mg USD 450.00 Ready to ship
500mg USD 950.00 Ready to ship
1g USD 1,650.00 Ready to Ship
2g USD 2,950.00 Ready to ship
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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
More Info
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.
Biological target:
Sotorasib is a KRAS G12C covalent inhibitor.
In vitro activity:
Sotorasib may have potential clinical use in combination with MEK and BCL-XL inhibitors in the treatment of patients with colorectal cancer exhibiting the G12C KRAS mutation. Sotorasib selectively exerted an antitumor effect on colon cancer cells with a G12C KRAS mutation. The combination of MEK and BCL-XL inhibition enhanced the effect of sotorasib in colon cancer cells. Reference: Mol Clin Oncol. 2021 Jul;15(1):148. https://pubmed.ncbi.nlm.nih.gov/34094546/
In vivo activity:
In immune-competent mice, treatment with sotorasib resulted in a pro-inflammatory tumour microenvironment and produced durable cures alone as well as in combination with immune-checkpoint inhibitors. Cured mice rejected the growth of isogenic KRASG12D tumours, which suggests adaptive immunity against shared antigens. Reference: Nature. 2019 Nov;575(7781):217-223. https://pubmed.ncbi.nlm.nih.gov/31666701/
Solvent mg/mL mM comments
Solubility
DMSO 75.0 133.78
Water 33.3 59.45
Ethanol 8.0 14.27
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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
Formulation protocol:
1. Huang M, Hou W, Zhang J, Li M, Zhang Z, Li X, Chen Z, Wang C, Yang L. Evaluation of AMG510 Therapy on KRAS-Mutant Non-Small Cell Lung Cancer and Colorectal Cancer Cell Using a 3D Invasive Tumor Spheroid System under Normoxia and Hypoxia. Bioengineering (Basel). 2022 Dec 12;9(12):792. doi: 10.3390/bioengineering9120792. PMID: 36550998; PMCID: PMC9774149. 2. Kitazawa M, Miyagawa Y, Koyama M, Nakamura S, Hondo N, Miyazaki S, Muranaka F, Tokumaru S, Yamamoto Y, Ehara T, Kuroiwa M, Tanaka H, Komatsu D, Takeoka M, Soejima Y. Drug sensitivity profile of minor KRAS mutations in colorectal cancer using mix culture assay: The effect of AMG-510, a novel KRAS G12C selective inhibitor, on colon cancer cells is markedly enhanced by the combined inhibition of MEK and BCL-XL. Mol Clin Oncol. 2021 Jul;15(1):148. doi: 10.3892/mco.2021.2310. Epub 2021 May 28. PMID: 34094546; PMCID: PMC8165703. 3. Takahashi Y, Tachi H, Watanabe R, Shimizu K, Yamamoto Y. Drug-induced lung injury in a patient treated with prior atezolizumab and subsequent sotorasib: A case report. Respirol Case Rep. 2024 Jan 24;12(1):e01284. doi: 10.1002/rcr2.1284. PMID: 38269310; PMCID: PMC10807503. 4. 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. PMID: 31666701.
In vitro protocol:
1. Huang M, Hou W, Zhang J, Li M, Zhang Z, Li X, Chen Z, Wang C, Yang L. Evaluation of AMG510 Therapy on KRAS-Mutant Non-Small Cell Lung Cancer and Colorectal Cancer Cell Using a 3D Invasive Tumor Spheroid System under Normoxia and Hypoxia. Bioengineering (Basel). 2022 Dec 12;9(12):792. doi: 10.3390/bioengineering9120792. PMID: 36550998; PMCID: PMC9774149. 2. Kitazawa M, Miyagawa Y, Koyama M, Nakamura S, Hondo N, Miyazaki S, Muranaka F, Tokumaru S, Yamamoto Y, Ehara T, Kuroiwa M, Tanaka H, Komatsu D, Takeoka M, Soejima Y. Drug sensitivity profile of minor KRAS mutations in colorectal cancer using mix culture assay: The effect of AMG-510, a novel KRAS G12C selective inhibitor, on colon cancer cells is markedly enhanced by the combined inhibition of MEK and BCL-XL. Mol Clin Oncol. 2021 Jul;15(1):148. doi: 10.3892/mco.2021.2310. Epub 2021 May 28. PMID: 34094546; PMCID: PMC8165703.
In vivo protocol:
1. Takahashi Y, Tachi H, Watanabe R, Shimizu K, Yamamoto Y. Drug-induced lung injury in a patient treated with prior atezolizumab and subsequent sotorasib: A case report. Respirol Case Rep. 2024 Jan 24;12(1):e01284. doi: 10.1002/rcr2.1284. PMID: 38269310; PMCID: PMC10807503. 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. PMID: 31666701.
1: Hondo N, Kitazawa M, Koyama M, Nakamura S, Tokumaru S, Miyazaki S, Kataoka M, Seharada K, Soejima Y. MEK inhibitor and anti-EGFR antibody overcome sotorasib resistance signals and enhance its antitumor effect in colorectal cancer cells. Cancer Lett. 2023 Jun 17:216264. doi: 10.1016/j.canlet.2023.216264. Epub ahead of print. PMID: 37336286. 2: Oya Y, Mitsudomi T. Is adagrasib just another sotorasib?-or, should we differentiate their usage according to patients' clinical presentation? Transl Lung Cancer Res. 2023 May 31;12(5):940-943. doi: 10.21037/tlcr-23-97. Epub 2023 May 8. PMID: 37323182; PMCID: PMC10261865. 3: Wu LL, Jiang WM, Liu ZY, Zhang YY, Qian JY, Liu Y, Huang YY, Li K, Li ZX, Ma GW, Xie D. AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research. Discov Oncol. 2023 Jun 7;14(1):91. doi: 10.1007/s12672-023-00698-z. PMID: 37284902; PMCID: PMC10247598. 4: Khan S, Budamagunta V, Zhou D. Targeting KRAS in pancreatic cancer: Emerging therapeutic strategies. Adv Cancer Res. 2023;159:145-184. doi: 10.1016/bs.acr.2023.02.004. Epub 2023 Mar 9. PMID: 37268395. 5: Potocki PM, Wójcik P, Chmura Ł, Goc B, Fedewicz M, Bielańska Z, Swadźba J, Konopka K, Kwinta Ł, Wysocki PJ. Clinical Characterization of Targetable Mutations (BRAF V600E and KRAS G12C) in Advanced Colorectal Cancer-A Nation-Wide Study. Int J Mol Sci. 2023 May 22;24(10):9073. doi: 10.3390/ijms24109073. PMID: 37240418; PMCID: PMC10219350. 6: Chour A, Denis J, Mascaux C, Zysman M, Bigay-Game L, Swalduz A, Gounant V, Cortot A, Darrason M, Fallet V, Auclin E, Basse C, Tissot C, Decroisette C, Bombaron P, Giroux-Leprieur E, Odier L, Brosseau S, Creusot Q, Gueçamburu M, Meersseman C, Rochand A, Costantini A, Gaillard CM, Wasielewski E, Girard N, Cadranel J, Lafitte C, Lebossé F, Duruisseaux M. Severe sotorasib-related hepatotoxicity and non-liver adverse events associated with sequential anti- PD(L)1 and sotorasib therapy in KRASG12C-mutant lung cancer. J Thorac Oncol. 2023 May 20:S1556-0864(23)00572-5. doi: 10.1016/j.jtho.2023.05.013. Epub ahead of print. PMID: 37217096. 7: Nagasaka M, Azmi AS. Penetrating the central nervous system sanctuary of KRAS, a target once thought "undruggable". Transl Lung Cancer Res. 2023 Apr 28;12(4):665-668. doi: 10.21037/tlcr-23-71. Epub 2023 Apr 6. PMID: 37197620; PMCID: PMC10183396. 8: Tria SM, Burge ME, Whitehall VLJ. The Therapeutic Landscape for KRAS-Mutated Colorectal Cancers. Cancers (Basel). 2023 Apr 19;15(8):2375. doi: 10.3390/cancers15082375. PMID: 37190303; PMCID: PMC10136970. 9: Lee C, Jiang ZK, Planken S, Manzuk LK, Ortiz R, Hall M, Noorbehesht K, Ram S, Affolter T, Troche GE, Ihle NT, Johnson T, Ahn Y, Kraus M, Giddabasappa A. Efficacy and Imaging Enabled Pharmacodynamic Profiling of KRAS G12C Inhibitors in Xenograft and Genetically Engineered Mouse Models of Cancer. Mol Cancer Ther. 2023 May 15:MCT-22-0810. doi: 10.1158/1535-7163.MCT-22-0810. Epub ahead of print. PMID: 37186518. 10: Wang A, Liu J, Li X, Zou F, Qi Z, Qi S, Liu Q, Wang Z, Cao J, Jiang Z, Wang B, Ge J, Wang L, Wang W, Liu J, Liu Q. Discovery of a highly potent pan-RAF inhibitor IHMT-RAF-128 for cancer treatment. Eur J Pharmacol. 2023 Aug 5;952:175752. doi: 10.1016/j.ejphar.2023.175752. Epub 2023 May 8. PMID: 37164118. 11: Shi Z, Weng J, Niu H, Yang H, Liu R, Weng Y, Zhu Q, Zhang Y, Tao L, Wang Z, Huh SJ, Jiang Y, Mei H, Dai X, Zhang L, Wang Y. D-1553: A novel KRASG12C inhibitor with potent and selective cellular and in vivo antitumor activity. Cancer Sci. 2023 May 9. doi: 10.1111/cas.15829. Epub ahead of print. PMID: 37158138. 12: Ito T, Oi I, Saito Z, Imakita T, Kanai O, Fujita K, Tachibana H, Moriyoshi K, Mio T. De Novo SCLC Transformation From KRAS G12C-Mutated Lung Adenocarcinoma With Excellent Response to Sotorasib: A Case Report. JTO Clin Res Rep. 2023 Mar 29;4(5):100510. doi: 10.1016/j.jtocrr.2023.100510. PMID: 37131995; PMCID: PMC10149245. 13: Tammaccaro SL, Prigent P, Le Bail JC, Dos-Santos O, Dassencourt L, Eskandar M, Buzy A, Venier O, Guillemot JC, Veeranagouda Y, Didier M, Spanakis E, Kanno T, Cesaroni M, Mathieu S, Canard L, Casse A, Windenberger F, Calvet L, Noblet L, Sidhu S, Debussche L, Moll J, Valtingojer I. TEAD Inhibitors Sensitize KRASG12C Inhibitors via Dual Cell Cycle Arrest in KRASG12C-Mutant NSCLC. Pharmaceuticals (Basel). 2023 Apr 6;16(4):553. doi: 10.3390/ph16040553. PMID: 37111311; PMCID: PMC10142471. 14: Zhou X, Ji Y, Zhou J. Multiple Strategies to Develop Small Molecular KRAS Directly Bound Inhibitors. Molecules. 2023 Apr 21;28(8):3615. doi: 10.3390/molecules28083615. PMID: 37110848; PMCID: PMC10146153. 15: Brazel D, Kim J, Ou SI. CodeBreaK 200: Sotorasib (AMG510) Has Broken the KRAS G12C+ NSCLC Enigma Code. Lung Cancer (Auckl). 2023 Apr 20;14:31-39. doi: 10.2147/LCTT.S403614. PMID: 37101896; PMCID: PMC10124743. 16: Zhang SS, Lee A, Nagasaka M. CodeBreak 200: Sotorasib Has Not Broken the KRASG12C Enigma Code. Lung Cancer (Auckl). 2023 Apr 19;14:27-30. doi: 10.2147/LCTT.S403461. PMID: 37101895; PMCID: PMC10123019. 17: Dy GK, Govindan R, Velcheti V, Falchook GS, Italiano A, Wolf J, Sacher AG, Takahashi T, Ramalingam SS, Dooms C, Kim DW, Addeo A, Desai J, Schuler M, Tomasini P, Hong DS, Lito P, Tran Q, Jones S, Anderson A, Hindoyan A, Snyder W, Skoulidis F, Li BT. Long-Term Outcomes and Molecular Correlates of Sotorasib Efficacy in Patients With Pretreated KRAS G12C-Mutated Non-Small-Cell Lung Cancer: 2-Year Analysis of CodeBreaK 100. J Clin Oncol. 2023 Jun 20;41(18):3311-3317. doi: 10.1200/JCO.22.02524. Epub 2023 Apr 25. PMID: 37098232. 18: Hamilton G, Stickler S, Rath B. Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras. Curr Pharm Des. 2023 Apr 18. doi: 10.2174/1381612829666230418114520. Epub ahead of print. PMID: 37073657. 19: Babu Manoharan G, Guzmán C, Najumudeen AK, Abankwa D. Detection of Ras nanoclustering-dependent homo-FRET using fluorescence anisotropy measurements. Eur J Cell Biol. 2023 Apr 11;102(2):151314. doi: 10.1016/j.ejcb.2023.151314. Epub ahead of print. PMID: 37058825. 20: Khan HY, Nagasaka M, Aboukameel A, Alkhalili O, Uddin MH, Bannoura S, Mzannar Y, Azar I, Beal E, Tobon M, Kim S, Beydoun R, Baloglu E, Senapedis W, El-Rayes B, Philip PA, Mohammad RM, Shields AF, Al-Hallak MN, Azmi AS. Anticancer efficacy of KRASG12C inhibitors is potentiated by PAK4 inhibitor KPT9274 in preclinical models of KRASG12C mutant pancreatic and lung cancers. bioRxiv [Preprint]. 2023 Mar 27:2023.03.27.534309. doi: 10.1101/2023.03.27.534309. PMID: 37034616; PMCID: PMC10081231.

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