WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206025
CAS#: 477588-78-6 (free base)
Description: ZK-304709 is a potent multi-target tumor growth inhibitor with IC50 = nanomolar inhibitory activity to cyclin-dependent kinases 1, 2, 4, 7 and 9, as well as vascular endothelial growth factor receptor tyrosine kinase 1-3 and of platelet-derived growth factor receptor beta tyrosine kinase.
Hodoodo Cat#: H206025
Name: ZK-304709
CAS#: 477588-78-6 (free base)
Chemical Formula: C13H16BrN5O3S
Exact Mass: 401.02
Molecular Weight: 402.270
Elemental Analysis: C, 38.82; H, 4.01; Br, 19.86; N, 17.41; O, 11.93; S, 7.97
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Related CAS #: 1010440-84-2 (HCl) 477588-78-6 (free base)
Synonym: ZK304709; ZK 304709; ZK304709; ZK CDK;
IUPAC/Chemical Name: (S)-4-((5-bromo-4-((1-hydroxypropan-2-yl)amino)pyrimidin-2-yl)amino)benzenesulfonamide
InChi Key: MJIALGDLOLWBRQ-QMMMGPOBSA-N
InChi Code: InChI=1S/C13H16BrN5O3S/c1-8(7-20)17-12-11(14)6-16-13(19-12)18-9-2-4-10(5-3-9)23(15,21)22/h2-6,8,20H,7H2,1H3,(H2,15,21,22)(H2,16,17,18,19)/t8-/m0/s1
SMILES Code: O=S(C1=CC=C(NC2=NC=C(Br)C(N[C@@H](C)CO)=N2)C=C1)(N)=O
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, not in water
Shelf Life: >5 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: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 402.27 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.
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: |
1: Scott EN, Thomas AL, Molife LR, Ahmed S, Blagden S, Fong PC, Kowal K, McCoy C, Wiesinger H, Steward W, De Bono J. A phase I dose escalation study of the pharmacokinetics and tolerability of ZK 304709, an oral multi-targeted growth inhibitor (MTGI), in patients with advanced solid tumours. Cancer Chemother Pharmacol. 2009 Jul;64(2):425-9. doi: 10.1007/s00280-009-0968-y. Epub 2009 Mar 12. PubMed PMID: 19280191.
2: Scholz A, Wagner K, Welzel M, Remlinger F, Wiedenmann B, Siemeister G, Rosewicz S, Detjen KM. The oral multitarget tumour growth inhibitor, ZK 304709, inhibits growth of pancreatic neuroendocrine tumours in an orthotopic mouse model. Gut. 2009 Feb;58(2):261-70. doi: 10.1136/gut.2007.146415. Epub 2008 Oct 1. PubMed PMID: 18829975.
3: Graham JS, Plummer R, McCoy C, Kowal K, Wiesinger H, Detjen K, Calvert H, Wiedenmann B, Cassidy J. Open-label, non-randomised, inter-individual dose escalation of ZK 304709 with the evaluation of safety, tolerability, pharmacokinetics, oral bioavailability and orientating efficacy after daily administration in patients with advanced cancer (7 d treatment and 14 d recovery). Eur J Cancer. 2008 Oct;44(15):2162-8. doi: 10.1016/j.ejca.2008.06.006. Epub 2008 Jul 22. PubMed PMID: 18653327.
4: Siemeister G, Luecking U, Wagner C, Detjen K, Mc Coy C, Bosslet K. Molecular and pharmacodynamic characteristics of the novel multi-target tumor growth inhibitor ZK 304709. Biomed Pharmacother. 2006 Jul;60(6):269-72. Epub 2006 Jun 23. PubMed PMID: 16887322.