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Chemical Structure| 2252403-56-6 Chemical Structure| 2252403-56-6

Structure of Sotorasib racemate
CAS No.: 2252403-56-6

Chemical Structure| 2252403-56-6

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AMG-510 is a covalent inhibitor of K-RAS(G12C) with antineoplastic activity.

Synonyms: AMG-510 racemate

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Product Details of Sotorasib racemate

CAS No. :2252403-56-6
Formula : C30H30F2N6O3
M.W : 560.59
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
Synonyms :
AMG-510 racemate
MDL No. :N/A
InChI Key :NXQKSXLFSAEQCZ-SFHVURJKSA-N
Pubchem ID :137278711

Safety of Sotorasib racemate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Sotorasib racemate

GPCR
MAPK
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
LU99 5 µM 2 monthourss Establish sotorasib-resistant cell lines to study resistance mechanisms. Resistant cells exhibited enhanced cell-matrix adhesion and activation of PAK and PI3K pathways. Br J Cancer. 2023 Jan;128(1):148-159
LU65 5 µM 2 monthourss Establish sotorasib-resistant cell lines to study resistance mechanisms. Resistant cells exhibited enhanced cell-matrix adhesion and activation of PAK and PI3K pathways. Br J Cancer. 2023 Jan;128(1):148-159
MIA PaCa-2 5 µM 2 monthourss Establish sotorasib-resistant cell lines to study resistance mechanisms. Resistant cells exhibited enhanced cell-matrix adhesion and activation of PAK and PI3K pathways. Br J Cancer. 2023 Jan;128(1):148-159
T24 16 µM 24 hours No inhibition of glucose metabolism observed Am J Cancer Res. 2024 Nov 15;14(11):5251-5268
UMUC3 16 µM 24 hours Inhibition of glucose metabolism Am J Cancer Res. 2024 Nov 15;14(11):5251-5268
SW1463 100 nM 4 to 72 hours Evaluate the inhibitory effect of KRASG12C inhibitors on the MAPK pathway and adaptive feedback reactivation Cell Rep. 2022 Jun 21;39(12):110993
MIA PaCa-2 100 nM 4 to 72 hours Evaluate the inhibitory effect of KRASG12C inhibitors on the MAPK pathway and adaptive feedback reactivation Cell Rep. 2022 Jun 21;39(12):110993
H358 100 nM 4 to 72 hours Evaluate the inhibitory effect of KRASG12C inhibitors on the MAPK pathway and adaptive feedback reactivation Cell Rep. 2022 Jun 21;39(12):110993
LU65 5 µM 4-6 weeks Establish sotorasib-resistant lung cancer cell lines and observe their growth and death after drug withdrawal. J Biomed Sci. 2023 Jun 29;30(1):50.
NCI-H23 5 µM 4-6 weeks Establish sotorasib-resistant lung cancer cell lines and observe their growth and death after drug withdrawal. J Biomed Sci. 2023 Jun 29;30(1):50.
MIA PaCa-2 5 µM 4-6 weeks Establish sotorasib-resistant pancreatic cancer cell lines and observe their growth and death after drug withdrawal. J Biomed Sci. 2023 Jun 29;30(1):50.
H9c2 cells 0, 7.5, 15, 30, 60 µM 48 hours To evaluate the effect of Sotorasib on cardiomyocyte viability, results showed Sotorasib significantly reduced cell viability. Cell Death Discov. 2025 Apr 12;11(1):169
CCC-HEH-2 cells 0, 7.5, 15, 30, 60 µM 48 hours To evaluate the effect of Sotorasib on cardiomyocyte viability, results showed Sotorasib significantly reduced cell viability. Cell Death Discov. 2025 Apr 12;11(1):169
SW1573 9.6 µM (IC50) 72 hours To evaluate the inhibitory effect of Sotorasib on SW1573 cells, results showed that SW1573 cells were inherently resistant to Sotorasib. Sci Adv. 2023 Oct 13;9(41):eade3816
H23 3.2 µM (IC50) 72 hours To evaluate the inhibitory effect of Sotorasib on H23 cells, results showed that H23 cells were tolerant to Sotorasib. Sci Adv. 2023 Oct 13;9(41):eade3816
H358 0.13 µM (IC50) 72 hours To evaluate the inhibitory effect of Sotorasib on H358 cells, results showed that H358 cells were highly sensitive to Sotorasib. Sci Adv. 2023 Oct 13;9(41):eade3816

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice UMUC3 and T24 xenograft models Gavage 10 mg/kg Every 2 days for 14 days Inhibition of KRASG12C mutant bladder tumor growth and expression of glucose metabolism-related proteins Am J Cancer Res. 2024 Nov 15;14(11):5251-5268
NOD/SCID mice Subcutaneous xenograft model Oral gavage 10 mg/kg Sotorasib, 30 mg/kg Alpelisib, 70 mg/kg FRAX597 Daily for 14 days Evaluate the antitumor effects of Sotorasib in combination with PAK inhibitor FRAX597 or PI3K inhibitor Alpelisib. Combination therapy significantly inhibited tumor growth. Br J Cancer. 2023 Jan;128(1):148-159
NOD/SCID mice Subcutaneous xenograft model Oral 10 mg/kg/day (Sotorasib), 20 mg/kg/day (Encorafenib) Daily administration for 14 days Evaluate the effect of sotorasib withdrawal and BRAF inhibitor combination on tumor growth. J Biomed Sci. 2023 Jun 29;30(1):50.
Mice Human tumor xenograft models Oral 100 mg/kg Once daily for 21-28 days Evaluate the anti-tumor effect of KRASG12C inhibitors in vivo and the combined therapeutic effect with EGFR or MEK inhibitors Cell Rep. 2022 Jun 21;39(12):110993
NSG mice PDO metastasis model (intracardiac injection) Intraperitoneal 100 mg/kg Daily administration for 5 months Evaluate the inhibitory effect of Sotorasib on PDO metastasis. Results showed no metastatic lesions in Sotorasib-treated mice (85% PDO_12 and 37% PDO_23 developed metastases in controls). Cell Rep Med. 2024 Oct 15;5(10):101777
Mice PDX model Oral and intraperitoneal injection 100mg/kg AMG510, 50mg/kg cetuximab AMG510 once daily, cetuximab twice weekly Evaluate the effect of AMG510 and cetuximab combination therapy, results showed significant tumor growth inhibition Cancer Discov. 2020 Aug;10(8):1129-1139
Mice SW1573 cell xenograft model Oral gavage 2.5 mg/kg or 5 mg/kg Twice a week for 16 weeks To evaluate the antitumor effects of Sotorasib alone or in combination with CFZ in the SW1573 cell xenograft model. Results showed that the combination of Sotorasib and CFZ significantly inhibited tumor growth and improved mouse survival. Sci Adv. 2023 Oct 13;9(41):eade3816
C57BL/6J mice Cardiac injury model Intragastric administration 300 mg/kg/d or 600 mg/kg/d Once daily for 28 days To evaluate the effect of Sotorasib on cardiac function in mice, results showed Sotorasib caused cardiac dysfunction, myocardial injury, and fibrosis. Cell Death Discov. 2025 Apr 12;11(1):169
Mice H358, MIA PaCa-2, and SW837 xenograft models DT2216 intraperitoneal injection, Sotorasib oral DT2216 15 mg/kg, Sotorasib 10 mg/kg DT2216 every four days, Sotorasib five days a week, continuous treatment Evaluated the antitumor efficacy of sotorasib alone or in combination with DT2216 in KRASG12C-mutated xenograft models, showing that the combination significantly inhibited tumor growth. J Hematol Oncol. 2022 Mar 9;15(1):23

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.92mL

1.78mL

0.89mL

17.84mL

3.57mL

1.78mL

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