WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H558243
CAS#: 869650-21-5
Description: K00135 is a potent and selective inhibitor of PIM kinases. K00135 was shown to impair survival and clonogenic growth of a panel of human acute leukemia cells. Exposure to K00135 also significantly suppressed in vitro growth of leukemic blasts from five acute myelogenous leukemia patients but not of normal umbilical cord blood mononuclear cells.
Hodoodo Cat#: H558243
Name: K00135
CAS#: 869650-21-5
Chemical Formula: C18H18N4O
Exact Mass: 306.15
Molecular Weight: 306.360
Elemental Analysis: C, 70.57; H, 5.92; N, 18.29; O, 5.22
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Synonym: K00135; K-00135; K 00135;
IUPAC/Chemical Name: 1-[3-[6-[(Cyclopropylmethyl)amino]imidazo[1,2-b]pyridazin-3-yl]phenyl]-ethanone
InChi Key: IVUBNTNWKIPCPS-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H18N4O/c1-12(23)14-3-2-4-15(9-14)16-11-20-18-8-7-17(21-22(16)18)19-10-13-5-6-13/h2-4,7-9,11,13H,5-6,10H2,1H3,(H,19,21)
SMILES Code: CC(C1=CC=CC(C2=CN=C3C=CC(NCC4CC4)=NN32)=C1)=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
Shelf Life: >2 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 306.36 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: Darby RA, Unsworth A, Knapp S, Kerr ID, Callaghan R. Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors. Cancer Chemother Pharmacol. 2015 Oct;76(4):853-64. doi: 10.1007/s00280-015-2858-9. Epub 2015 Sep 9. PubMed PMID: 26351135.
2: Yan B, Yau EX, Samanta S, Ong CW, Yong KJ, Ng LK, Bhattacharya B, Lim KH, Soong R, Yeoh KG, Deng N, Tan P, Lam Y, Salto-Tellez M; Singapore Gastric Cancer Consortium. Clinical and therapeutic relevance of PIM1 kinase in gastric cancer. Gastric Cancer. 2012 Apr;15(2):188-97. doi: 10.1007/s10120-011-0097-2. Epub 2011 Oct 13. PubMed PMID: 21993851.
3: Pogacic V, Bullock AN, Fedorov O, Filippakopoulos P, Gasser C, Biondi A, Meyer-Monard S, Knapp S, Schwaller J. Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. Cancer Res. 2007 Jul 15;67(14):6916-24. PubMed PMID: 17638903.
4: Taparowsky EJ, Gerbi SA. Structure of 1.71 lb gm/cm(3) bovine satellite DNA: evolutionary relationship to satellite I. Nucleic Acids Res. 1982 Sep 25;10(18):5503-15. PubMed PMID: 6292843; PubMed Central PMCID: PMC320891.
