MedKoo Cat#: 598192 | Name: Govitecan

Description:

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

Govitecan (also known as SN-38 or in its prodrug conjugated form, sacituzumab govitecan) is a potent topoisomerase I inhibitor and the active metabolite of irinotecan. In preclinical studies, SN-38 exhibits nanomolar cytotoxic activity against a wide range of tumor cell lines, with IC₅₀ values typically ranging from 0.1 to 10 nM. Sacituzumab govitecan, an antibody-drug conjugate (ADC) linking SN-38 to an anti-Trop-2 monoclonal antibody via a hydrolyzable linker, delivers targeted cytotoxicity to Trop-2–expressing tumors.

Chemical Structure

Govitecan
Govitecan
CAS#1918106-06-5

Theoretical Analysis

MedKoo Cat#: 598192

Name: Govitecan

CAS#: 1918106-06-5

Chemical Formula: C73H99N11O22

Exact Mass: 1481.6966

Molecular Weight: 1482.65

Elemental Analysis: C, 59.14; H, 6.73; N, 10.39; O, 23.74

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1918106-06-5 1469876-18-3
Synonym
Govitecan; SN-38-linker.
IUPAC/Chemical Name
Carbonic acid, [4-[[(2S)-2-(4-aminobutyl)-35-[4-[[[[4-[(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)methyl]cyclohexyl]carbonyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-1,4,8-trioxo-6,12,15,18,21,24,27,30,33-nonaoxa-3,9-diazapentatriacont-1-yl]amino]phenyl]methyl (4S)-4,11-diethyl-3,4,5b,6,12,14-hexahydro-9-hydroxy-3,14-dioxo-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinolin-4-yl ester
InChi Key
WYTMLZHQEXUPEH-HASCFQAKSA-N
InChi Code
InChI=1S/C73H99N11O22/c1-3-55-56-39-54(85)16-17-60(56)79-67-57(55)44-83-62(67)40-59-58(70(83)92)46-104-71(93)73(59,4-2)106-72(94)105-45-50-10-14-52(15-11-50)77-69(91)61(7-5-6-20-74)78-64(87)48-103-47-63(86)75-21-23-95-25-27-97-29-31-99-33-35-101-37-38-102-36-34-100-32-30-98-28-26-96-24-22-82-43-53(80-81-82)41-76-68(90)51-12-8-49(9-13-51)42-84-65(88)18-19-66(84)89/h10-11,14-19,39-40,43,49,51,61,67,79,85H,3-9,12-13,20-38,41-42,44-48,74H2,1-2H3,(H,75,86)(H,76,90)(H,77,91)(H,78,87)/t49?,51?,61-,67?,73-/m0/s1
SMILES Code
O=C(O[C@](C1=C(CO2)C(N3CC4=C(CC)C5=C(NC4C3=C1)C=CC(O)=C5)=O)(CC)C2=O)OCC6=CC=C(NC([C@H](CCCCN)NC(COCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCN7N=NC(CNC(C8CCC(CN9C(C=CC9=O)=O)CC8)=O)=C7)=O)=O)=O)C=C6
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
2934.99.03.00
More Info
In clinical trials, sacituzumab govitecan has demonstrated objective response rates of ~33% and progression-free survival of ~5.5 months in metastatic triple-negative breast cancer (mTNBC) patients refractory to prior therapies. The bioactivity profile of govitecan is marked by a high drug-to-antibody ratio (DAR ~7–8), sustained tumor exposure, and selective delivery that enhances antitumor efficacy while mitigating systemic toxicity compared to free SN-38.

Preparing Stock Solutions

The following data is based on the product molecular weight 1,482.65 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
1: Dotan E, Cohen SJ, Starodub AN, Lieu CH, Messersmith WA, Simpson PS, Guarino MJ, Marshall JL, Goldberg RM, Hecht JR, Wegener WA, Sharkey RM, Govindan SV, Goldenberg DM, Berlin JD. Phase I/II Trial of Labetuzumab Govitecan (Anti-CEACAM5/SN-38 Antibody-Drug Conjugate) in Patients With Refractory or Relapsing Metastatic Colorectal Cancer. J Clin Oncol. 2017 Oct 10;35(29):3338-3346. doi: 10.1200/JCO.2017.73.9011. Epub 2017 Aug 17. PubMed PMID: 28817371.