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Cayman Garsorasib, 1 mg


Product Description
Garsorasib is an inhibitor of K-Ras containing the activating glycine-to-cysteine mutation at position 12 (K-RasG12C; IC50 = 18 nM).1 It selectively binds to GDP-bound K-RasG12C over GDP-bound wild-type K-Ras in thermal shift assays and selectively inhibits ERK phosphorylation in NCI H358 cells, which express K-RasG12C, over NCI H1993 cells, which express wild-type K-Ras (IC50s = 6.9 and >1,000 nM, respectively). Garsorasib inhibits proliferation in 11 K-RasG12C-expressing cancer cell lines (IC50s = 4.6-33 nM) but not in K-RasG12D- or wild-type-expressing cancer cells (IC50s = >10,000 nM). In vivo, garsorasib (30 mg/kg) induces tumor regression in NCI H358 non-small cell lung cancer (NSCLC) and MIA PaCa-2 pancreatic cancer mouse xenograft models.
WARNING This product is not for human or veterinary use.
Technical Information
| Formal Name | 7-(2-amino-6-fluorophenyl)-1-(4, 6-dicyclopropyl-5-pyrimidinyl)-4-[(2S,5R)-2,5-dimethyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-6-fluoro-pyrido[2,3-d]pyrimidin-2(1H)-one |
| CAS Number | 2559761-14-5 |
| Synonyms |
|
| Molecular Formula | C32H32F2N8O2 |
| Formula Weight | 598.7 |
| Purity | ≥98% |
| Formulation(Request formulation change) | A solid |
| Solubility(Learn about Variance in Solubility) | Acetonitrile: Slightly soluble: 0.1-1 mg/mLDMSO: Slightly soluble: 0.1-1 mg/mL |
| SMILES | O=C1N(C2=NC(C3=C(C=CC=C3N)F)=C(F)C=C2C(N4[C@H](CN([C@@H](C4)C)C(C=C)=O)C)=N1)C5=C(C6CC6)N=CN=C5C7CC7 |
| 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 |
| InChi Key | DKFRWZJCNPETGI-SJORKVTESA-N |
Shipping & Storage Information
| Storage | -20°C |
| Shipping | Room temperature in continental US; may vary elsewhere |
| Stability | ≥ 4 years |
| SKU | CAYM-44250-1 |
|---|---|
| Supplier Part Number | 44250-1 |
| UM | EA |
| UNSPSC | 41116107 |
| Manufacturer | Cayman |
| Temperature | -20 |
| Refrigerated-Frozen | Y |
| CountryOfOrigin | United States |
| ProductLine | CAYM |
| Qty | 1 |
| MinOrderQty | 1 |
| Weight | 7.000000 |
| Lead Time | 5 |
| Hazardous | N |
| CAS Number | 2559761-14-5 |
| Energy Star | No |
| Green | No |
| Controlled | N |

