Garsorasib
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MedKoo CAT#: 577748

CAS#: 2559761-14-5

Description: Garsorasib, also known as D-1553, is a potent and selective oral KRASG12C inhibitor. D-1553 showed selective and potent activity against mutated GDP-bound KRASG12C protein. D-1553 selectively inhibited ERK phosphorylation in NCI-H358 cells harboring KRASG12C mutation. Compared to the KRAS WT and KRASG12D cell lines, D-1553 selectively inhibited cell viability in multiple KRASG12C cell lines, and the potency was slightly superior to sotorasib and adagrasib. In a panel of xenograft tumor models, D-1553, given orally, showed partial or complete tumor regression. The combination of D-1553 with chemotherapy, MEK inhibitor, or SHP2 inhibitor showed stronger potency on tumor growth inhibition or regression compared to D-1553 alone.


Chemical Structure

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Garsorasib
CAS# 2559761-14-5

Theoretical Analysis

MedKoo Cat#: 577748
Name: Garsorasib
CAS#: 2559761-14-5
Chemical Formula: C32H32F2N8O2
Exact Mass: 598.26
Molecular Weight: 598.660
Elemental Analysis: C, 64.20; H, 5.39; F, 6.35; N, 18.72; O, 5.34

Price and Availability

Size Price Availability Quantity
5mg USD 850 2 Weeks
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Synonym: Garsorasib; D-1553; D 1553; D1553;

IUPAC/Chemical Name: 7-(2-amino-6-fluorophenyl)-1-(4,6-dicyclopropylpyrimidin-5-yl)-4-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-6-fluoropyrido[2,3-d]pyrimidin-2(1H)-one

InChi Key: DKFRWZJCNPETGI-SJORKVTESA-N

InChi Code: InChI=1S/C32H32F2N8O2/c1-4-24(43)40-13-17(3)41(14-16(40)2)30-20-12-22(34)28(25-21(33)6-5-7-23(25)35)38-31(20)42(32(44)39-30)29-26(18-8-9-18)36-15-37-27(29)19-10-11-19/h4-7,12,15-19H,1,8-11,13-14,35H2,2-3H3/t16-,17+/m1/s1

SMILES Code: O=C1N(C2=C(C3CC3)N=CN=C2C4CC4)C5=NC(C6=C(F)C=CC=C6N)=C(F)C=C5C(N7[C@@H](C)CN(C(C=C)=O)[C@H](C)C7)=N1

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 598.66 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:
In vitro protocol:
In vivo protocol:

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1: 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 Jul;114(7):2951-2960. doi: 10.1111/cas.15829. Epub 2023 May 9. PMID: 37158138; PMCID: PMC10323112.


2: Li Z, Song Z, Zhao Y, Wang P, Jiang L, Gong Y, Zhou J, Jian H, Dong X, Zhuang W, Cang S, Yang N, Fang J, Shi J, Lu J, Ma R, Wu P, Zhang Y, Song M, Xu CW, Shi Z, Zhang L, Wang Y, Wang X, Zhang Y, Lu S. D-1553 (Garsorasib), a Potent and Selective Inhibitor of KRASG12C in Patients With NSCLC: Phase 1 Study Results. J Thorac Oncol. 2023 Jul;18(7):940-951. doi: 10.1016/j.jtho.2023.03.015. Epub 2023 Mar 21. PMID: 36948246.