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Setidegrasib (ASP3082) PROTAC chemical

Cat.No.E4757

ASP3082 (Setidegrasib; KRAS G12D inhibitor 17) is a PROTAC degrader targeting KRAS(G12D) with a DC50 of 38 nM. It effectively inhibits growth in various KRAS(G12D)-mutated cancer cell lines, including pancreatic (PK-59, HPAC) and colorectal (GP2d, GP5d) with IC50 values ranging from 3.6 to 29 nM.

Chemical Structure

Molecular Weight: 1117.30

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Quality Control

Batch: E475701 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.81%
99.81

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (89.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 1117.30 Formula

C60H65FN12O7S

 Storage (From the date of receipt)
CAS No. 2821793-99-9 Download SDF Download SDF Storage of Stock Solutions

Synonyms ASP-3082; KRAS G12D inhibitor 17 Smiles CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)C)N4C=C(N=N4)C5=CC=C(C=C5)COC6=[C@]([C@]7=C(C(F)=CC8=C7C=NN8)C)C(C9CC9)=CC%10=C6N=C(N=C%10N%11C[C@@H]%12C[C@H]%11CN%12)OC%13CCOCC%13)=O)O)=O)CO

Mechanism of Action

In vivo

Setidegrasib (ASP3082) exhibits dose-dependent anti-tumor activity in PK-59, LXFA 1125 NSCLC PDX, AsPC-1 (pancreatic) and GP2d (colorectal) KRAS(G12D)-mutated xenograft models of Balb/c nu/nu nude mice at doses of 0.3–30 mg/kg (i.v., once/twice weekly, 14–22 days).
References

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