RP03707 | KRASG12D degrader

MedKoo Cat#: 128900 | Name: RP03707

Description:

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

RP03707 is a CRBN-involving, highly potent, and selective KRASG12D degrader. RP03707 effectively inhibits tumor cell growth in multiple KRASG12D cell lines. It also exhibits prolonged PK/PD effects and excellent efficacy in mouse CDX models bearing KRASG12D tumors.

Chemical Structure

RP03707

CAS#N/A

Theoretical Analysis

MedKoo Cat#: 128900

Name: RP03707

CAS#: N/A

Chemical Formula: C55H58F3N11O4

Exact Mass: 993.4625

Molecular Weight: 994.14

Elemental Analysis: C, 66.45; H, 5.88; F, 5.73; N, 15.50; O, 6.44

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.

Bulk Inquiry

Related CAS #

No Data

Synonym

RP03707; RP-03707; RP 03707

IUPAC/Chemical Name

1-(6-(1-(7-((1-(((4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-7-(8-ethynyl-7-fluoro-3-hydroxynaphthalen-1-yl)-8-fluoropyrido[4,3-d]pyrimidin-2-yl)oxy)methyl)cyclopropyl)methyl)-7-azaspiro[3.5]nonan-2-yl)piperidin-4-yl)-5-fluoro-1-methyl-1H-indazol-3-yl)dihydropyrimidine-2,4(1H,3H)-dione

InChi Key

PLUHAAKDSAEFSC-UHFFFAOYSA-N

InChi Code

InChI=1S/C55H58F3N11O4/c1-3-37-42(56)7-4-32-20-36(70)21-40(46(32)37)48-47(58)49-41(26-59-48)50(68-27-33-5-6-34(28-68)60-33)63-52(62-49)73-30-55(11-12-55)29-66-18-13-54(14-19-66)24-35(25-54)67-15-8-31(9-16-67)38-23-44-39(22-43(38)57)51(64-65(44)2)69-17-10-45(71)61-53(69)72/h1,4,7,20-23,26,31,33-35,60,70H,5-6,8-19,24-25,27-30H2,2H3,(H,61,71,72)

SMILES Code

OC(C=C1C2=C(F)C(N=C(OCC3(CC3)CN4CCC5(CC(N6CCC(C7=CC(N(C)N=C8N9CCC(NC9=O)=O)=C8C=C7F)CC6)C5)CC4)N=C%10N%11CC%12NC(CC%12)C%11)=C%10C=N2)=CC%13=C1C(C#C)=C(F)C=C%13

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 994.14 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

Discovery and Characterization of RP03707: A Highly Potent and Selective KRASG12D PROTAC Xiang Ji, Huanping Li, Gang Wu, Qiguo Zhang, Xiaolin He, Yanpeng Wu, Bin Zong, Xiaojin Xu, Chao Liang, Beibei Wang, Yuwei Zhang, Qingyao Hu, Chao Deng, Liqiang Shen, Zijun Chen, Bing Bai, Lin Wang, Jinchao Ai, Leduo Zhang, Honggui Zhou, Shihao Sun, Yijie Wang, Youhong Wang, Qiming Fan, Dawei Chen, Tianlun Zhou, Xianqi Kong, and Jiasheng Lu Journal of Medicinal Chemistry Article ASAP DOI: 10.1021/acs.jmedchem.5c00428