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MedKoo Cat#: 207020 | Name: DS-1205B
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Description:

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

DS-1205, also known as DS-1205b, is a selective and potent AXL kinase inhibitor with IC50 of 1.3 nM. DS-1205 potently inhibited the hGAS6-induced migration in vitro with EC50 of 2.7 nM. DS-1205b monotherapy exerted significant antitumor activity in an NIH3T3-AXL allograft model. In an HCC827 xenograft model, combination treatment with DS-1205b and osimertinib significantly delayed on the onset of tumor resistance compared to osimertinib alone in a manner proportional to DS-1205b does. DS-1205b also showed a similar resistance delay effect with erlotinib combination in the same xenograft model.

Chemical Structure

DS-1205B
DS-1205B
CAS#1855860-24-0 (free base)

Theoretical Analysis

MedKoo Cat#: 207020

Name: DS-1205B

CAS#: 1855860-24-0 (free base)

Chemical Formula: C41H42FN5O7

Exact Mass: 735.3068

Molecular Weight: 735.81

Elemental Analysis: C, 66.93; H, 5.75; F, 2.58; N, 9.52; O, 15.22

Price and Availability

Size Price Availability Quantity
10mg USD 850.00 2 Weeks
25mg USD 1,650.00 2 Weeks
50mg USD 2,650.00 2 Weeks
100mg USD 4,250.00 3 months
200mg USD 7,950.00 3 months
500mg USD 13,950.00 3 months
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Related CAS #
1855860-24-0 (free base) 1855861-49-2 (mesylate) 1855861-62-9 (phosphate) 1855861-63-0 (2 sulfate) 1855861-64-1 (1.5 sulfate) 2407835-63-4 (X sulfate)
Synonym
DS-1205; DS 1205; DS1205; DS-1205b; DS 1205b; DS1205b; DS-1206b
IUPAC/Chemical Name
(R)-N-(4-(5-(4-((1,4-dioxan-2-yl)methoxy)-3-methoxyphenyl)-2-aminopyridin-3-yl)-3-fluorophenyl)-5-methyl-4'-oxo-1'-((tetrahydro-2H-pyran-4-yl)methyl)-1',4'-dihydro-[2,3'-bipyridine]-5'-carboxamide
InChi Key
ZOEILZXFYPPMTR-SSEXGKCCSA-N
InChi Code
InChI=1S/C41H42FN5O7/c1-25-3-7-36(44-18-25)33-21-47(20-26-9-11-51-12-10-26)22-34(39(33)48)41(49)46-29-5-6-31(35(42)17-29)32-15-28(19-45-40(32)43)27-4-8-37(38(16-27)50-2)54-24-30-23-52-13-14-53-30/h3-8,15-19,21-22,26,30H,9-14,20,23-24H2,1-2H3,(H2,43,45)(H,46,49)/t30-/m1/s1
SMILES Code
CC1=CC=C(C2=CN(CC3CCOCC3)C=C(C(NC4=CC=C(C5=C(N)N=CC(C6=CC(OC)=C(OC[C@@H]7OCCOC7)C=C6)=C5)C(F)=C4)=O)C2=O)N=C1
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
2934.99.9001
More Info
AXL is a receptor tyrosine kinase that plays an important role in signal transduction in normal and malignant cells. Abnormal expression and/or activation of AXL can provide a survival advantage for certain cancer cells, and AXL up-regulation is associated with poor prognosis in several cancers. Recently, it has been reported that up-regulation of AXL expression is a mechanism of EGFR-TKI resistance in EGFR-mutant non-small cell lung cancer.
Product Data
Product Data
Instruction
View handling instruction
Biological target:
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively.
In vitro activity:
Thus, DS-1205b is a highly selective and potent AXL kinase inhibitor. DS-1205b showed potent and highly selective inhibitory activities toward AXL kinase. Reference: Oncotarget. 2019 Aug 27;10(50):5152-5167. https://pubmed.ncbi.nlm.nih.gov/31497246/
In vivo activity:
Tumors started to regrow after 48 days of treatment with erlotinib, and DS-1205b treatment was initiated at day 62. DS-1205b inhibited mouse tumor growth by 97% and 47% at doses of 50 and 25 mg/kg, respectively. A statistically significant antitumor effect was observed at each measurement point for DS-1205b at 50 mg/kg (P = 0.0100) (Figure 5B). Reference: Oncotarget. 2019 Aug 27;10(50):5152-5167. https://pubmed.ncbi.nlm.nih.gov/31497246/
Solvent mg/mL mM
Solubility
Soluble in DMSO 0.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 735.81 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:
1. Jimbo T, Hatanaka M, Komatsu T, Taira T, Kumazawa K, Maeda N, Suzuki T, Ota M, Haginoya N, Isoyama T, Fujiwara K. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167. doi: 10.18632/oncotarget.27114. PMID: 31497246; PMCID: PMC6718264.
In vitro protocol:
1. Jimbo T, Hatanaka M, Komatsu T, Taira T, Kumazawa K, Maeda N, Suzuki T, Ota M, Haginoya N, Isoyama T, Fujiwara K. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167. doi: 10.18632/oncotarget.27114. PMID: 31497246; PMCID: PMC6718264.
In vivo protocol:
1. Jimbo T, Hatanaka M, Komatsu T, Taira T, Kumazawa K, Maeda N, Suzuki T, Ota M, Haginoya N, Isoyama T, Fujiwara K. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167. doi: 10.18632/oncotarget.27114. PMID: 31497246; PMCID: PMC6718264.
Jimbo T, Hatanaka M, Komatsu T, et al. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019;10(50):5152–5167. Published 2019 Aug 27. doi:10.18632/oncotarget.27114